Grouped product items

SKU

Size

Availability

Price

Qty

N172464-1mg

1mg

Available within 8-12 weeks(?)

$44.90

N172464-5mg

5mg

Available within 8-12 weeks(?)

$124.90

N172464-10mg

10mg

Available within 8-12 weeks(?)

$199.90

N172464-25mg

25mg

Available within 8-12 weeks(?)

$399.90

Basic Description

Synonyms	Cipargamin\|1193314-23-6\|NITD609\|NITD 609\|NITD-609\|KAE609\|Cipargamin [INN]\|Spiro[3H-indole-3,1'-[1H]pyrido[3,4-b]indol]-2(1H)-one, 5,7'-dichloro-6'-fluoro-2',3',4',9'-tetrahydro-3'-methyl-, (1'R,3'S)-\|Z7Q4FWA04P\|(3R,3'S)-5,7'-dichloro-6'-fluoro-3'-methylsp
Specifications & Purity	Moligand™, ≥97%
Storage Temp	Store at -20°C
Shipped In	Ice chest + Ice pads
Grade	Moligand™
Action Type	INHIBITOR
Mechanism of action	P-type ATPase inhibitor
Product Description	Cipargamin (NITD609) is an potent antimalarial compound, with an IC50 of appr 1 nM against P. falciparum.

Product Properties

ALogP	3.9

Associated Targets

CNTLN Tbio Centlein 0 Activities

Discover Target: CNTLN

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CYP2D6 Tclin Cytochrome P450 2D6 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CNR1 Tclin Cannabinoid receptor 1 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

DRD1 Tclin D(1A) dopamine receptor 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

DRD2 Tclin D(2) dopamine receptor 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

DRD4 Tchem D(4) dopamine receptor 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CYP3A4 Tclin Cytochrome P450 3A4 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ESR1 Tclin Estrogen receptor 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

GABRA1 Tclin Gamma-aminobutyric acid receptor subunit alpha-1 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

NR3C1 Tclin Glucocorticoid receptor 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ESR2 Tclin Estrogen receptor beta 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AVPR1A Tclin Vasopressin V1a receptor 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HRH1 Tclin Histamine H1 receptor 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

SLC6A2 Tclin Sodium-dependent noradrenaline transporter 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

SLC6A3 Tclin Sodium-dependent dopamine transporter 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

SLC6A4 Tclin Sodium-dependent serotonin transporter 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PDE4D Tclin cAMP-specific 3',5'-cyclic phosphodiesterase 4D 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PDE3A Tclin cGMP-inhibited 3',5'-cyclic phosphodiesterase A 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PTGS1 Tclin Prostaglandin G/H synthase 1 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PTGS2 Tclin Prostaglandin G/H synthase 2 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CACNA1C Tclin Voltage-dependent L-type calcium channel subunit alpha-1C 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

DRD3 Tclin D(3) dopamine receptor 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CHRM3 Tclin Muscarinic acetylcholine receptor M3 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ADRA2B Tclin Alpha-2B adrenergic receptor 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CHRM2 Tclin Muscarinic acetylcholine receptor M2 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ADRA2C Tclin Alpha-2C adrenergic receptor 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HTR2A Tclin 5-hydroxytryptamine receptor 2A 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ADORA2A Tclin Adenosine receptor A2a 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CHRM1 Tclin Muscarinic acetylcholine receptor M1 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ADRA2A Tclin Alpha-2A adrenergic receptor 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ADRB1 Tclin Beta-1 adrenergic receptor 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ADRA1A Tclin Alpha-1A adrenergic receptor 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AR Tclin Androgen receptor 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MAOA Tclin Amine oxidase [flavin-containing] A 0 Activities

Discover Target: MAOA

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HTR2C Tclin 5-hydroxytryptamine receptor 2C 0 Activities

Discover Target: HTR2C

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HTR1A Tclin 5-hydroxytryptamine receptor 1A 0 Activities

Discover Target: HTR1A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ADORA3 Tchem Adenosine receptor A3 0 Activities

Discover Target: ADORA3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HTR3A Tclin 5-hydroxytryptamine receptor 3A 0 Activities

Discover Target: HTR3A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HTR2B Tclin 5-hydroxytryptamine receptor 2B 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

EDNRA Tclin Endothelin-1 receptor 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

EDNRB Tclin Endothelin receptor type B 0 Activities

Discover Target: EDNRB

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KCNH2 Tclin Potassium voltage-gated channel subfamily H member 2 0 Activities

Discover Target: KCNH2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

OPRD1 Tclin Delta-type opioid receptor 0 Activities

Discover Target: OPRD1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

OPRK1 Tclin Kappa-type opioid receptor 0 Activities

Discover Target: OPRK1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

OPRM1 Tclin Mu-type opioid receptor 0 Activities

Discover Target: OPRM1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

TACR1 Tclin Substance-P receptor 0 Activities

Discover Target: TACR1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MLNR Tchem Motilin receptor 0 Activities

Discover Target: MLNR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Names and Identifiers

IUPAC Name	(3R,3'S)-5,7'-dichloro-6'-fluoro-3'-methylspiro[1H-indole-3,1'-2,3,4,9-tetrahydropyrido[3,4-b]indole]-2-one
INCHI	InChI=1S/C19H14Cl2FN3O/c1-8-4-11-10-6-14(22)13(21)7-16(10)23-17(11)19(25-8)12-5-9(20)2-3-15(12)24-18(19)26/h2-3,5-8,23,25H,4H2,1H3,(H,24,26)/t8-,19+/m0/s1
InChi Key	CKLPLPZSUQEDRT-WPCRTTGESA-N
Canonical SMILES	CC1CC2=C(C3(N1)C4=C(C=CC(=C4)Cl)NC3=O)NC5=CC(=C(C=C25)F)Cl
Isomeric SMILES	C[C@H]1CC2=C([C@]3(N1)C4=C(C=CC(=C4)Cl)NC3=O)NC5=CC(=C(C=C25)F)Cl
PubChem CID	44469321
Molecular Weight	390.24

Database links

PubChem CID	44469321
Wikipedia	Cipargamin
ChEMBL Ligand	CHEMBL1082723
CAS Registry No.	1193314-23-6

Certificates

Certificate of Analysis(COA)

Enter Lot Number to search for COA:

To view the certificate results,please click on a Lot number.For Lot numbers from past orders,please use our order status section

4 results found

Lot Number	Certificate Type	Date	Item
H2419151	Certificate of Analysis	May 07, 2024	N172464
H2419152	Certificate of Analysis	May 07, 2024	N172464
H2419153	Certificate of Analysis	May 07, 2024	N172464
H2419154	Certificate of Analysis	May 07, 2024	N172464

References

1. Yeung BK, Zou B, Rottmann M, Lakshminarayana SB, Ang SH, Leong SY, Tan J, Wong J, Keller-Maerki S, Fischli C et al.. (2010) Spirotetrahydro beta-carbolines (spiroindolones): a new class of potent and orally efficacious compounds for the treatment of malaria.. J Med Chem, 53 (14): (5155-64). [PMID:20568778]
2. Rottmann M, McNamara C, Yeung BK, Lee MC, Zou B, Russell B, Seitz P, Plouffe DM, Dharia NV, Tan J et al.. (2010) Spiroindolones, a potent compound class for the treatment of malaria.. Science, 329 (5996): (1175-80). [PMID:20813948]
3. van Pelt-Koops JC, Pett HE, Graumans W, van der Vegte-Bolmer M, van Gemert GJ, Rottmann M, Yeung BK, Diagana TT, Sauerwein RW. (2012) The spiroindolone drug candidate NITD609 potently inhibits gametocytogenesis and blocks Plasmodium falciparum transmission to anopheles mosquito vector.. Antimicrob Agents Chemother, 56 (7): (3544-8). [PMID:22508309]
4. Spillman NJ, Allen RJ, McNamara CW, Yeung BK, Winzeler EA, Diagana TT, Kirk K. (2013) Na(+) regulation in the malaria parasite Plasmodium falciparum involves the cation ATPase PfATP4 and is a target of the spiroindolone antimalarials.. Cell Host Microbe, 13 (2): (227-37). [PMID:23414762]
5. White NJ, Pukrittayakamee S, Phyo AP, Rueangweerayut R, Nosten F, Jittamala P, Jeeyapant A, Jain JP, Lefèvre G, Li R et al.. (2014) Spiroindolone KAE609 for falciparum and vivax malaria.. N Engl J Med, 371 (5): (403-10). [PMID:25075833]
6. Stein DS, Jain JP, Kangas M, Lefèvre G, Machineni S, Griffin P, Lickliter J. (2015) Open-label, single-dose, parallel-group study in healthy volunteers to determine the drug-drug interaction potential between KAE609 (cipargamin) and piperaquine.. Antimicrob Agents Chemother, 59 (6): (3493-500). [PMID:25845867]
7. Goldgof GM, Durrant JD, Ottilie S, Vigil E, Allen KE, Gunawan F, Kostylev M, Henderson KA, Yang J, Schenken J et al.. (2016) Comparative chemical genomics reveal that the spiroindolone antimalarial KAE609 (Cipargamin) is a P-type ATPase inhibitor.. Sci Rep, 6 (3): (27806). [PMID:27291296]

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SKU	Size	Availability	Price
N172464-1mg	1mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$44.90
N172464-5mg	5mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$124.90
N172464-10mg	10mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$199.90
N172464-25mg	25mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$399.90

NITD-609 - 97%, high purity , P-type ATPase inhibitor, CAS No.1193314-23-6, P-type ATPase inhibitor

Basic Description

Product Properties

Associated Targets

CNTLN Tbio Centlein 0 Activities

CYP2D6 Tclin Cytochrome P450 2D6 0 Activities

CNR1 Tclin Cannabinoid receptor 1 0 Activities

DRD1 Tclin D(1A) dopamine receptor 0 Activities

DRD2 Tclin D(2) dopamine receptor 0 Activities

DRD4 Tchem D(4) dopamine receptor 0 Activities

CYP3A4 Tclin Cytochrome P450 3A4 0 Activities

ESR1 Tclin Estrogen receptor 0 Activities

GABRA1 Tclin Gamma-aminobutyric acid receptor subunit alpha-1 0 Activities

NR3C1 Tclin Glucocorticoid receptor 0 Activities

ESR2 Tclin Estrogen receptor beta 0 Activities

AVPR1A Tclin Vasopressin V1a receptor 0 Activities

HRH1 Tclin Histamine H1 receptor 0 Activities

SLC6A2 Tclin Sodium-dependent noradrenaline transporter 0 Activities

SLC6A3 Tclin Sodium-dependent dopamine transporter 0 Activities

SLC6A4 Tclin Sodium-dependent serotonin transporter 0 Activities

PDE4D Tclin cAMP-specific 3',5'-cyclic phosphodiesterase 4D 0 Activities

PDE3A Tclin cGMP-inhibited 3',5'-cyclic phosphodiesterase A 0 Activities

PTGS1 Tclin Prostaglandin G/H synthase 1 0 Activities

PTGS2 Tclin Prostaglandin G/H synthase 2 0 Activities

CACNA1C Tclin Voltage-dependent L-type calcium channel subunit alpha-1C 0 Activities

DRD3 Tclin D(3) dopamine receptor 0 Activities

CHRM3 Tclin Muscarinic acetylcholine receptor M3 0 Activities

ADRA2B Tclin Alpha-2B adrenergic receptor 0 Activities

CHRM2 Tclin Muscarinic acetylcholine receptor M2 0 Activities

ADRA2C Tclin Alpha-2C adrenergic receptor 0 Activities

HTR2A Tclin 5-hydroxytryptamine receptor 2A 0 Activities

ADORA2A Tclin Adenosine receptor A2a 0 Activities

CHRM1 Tclin Muscarinic acetylcholine receptor M1 0 Activities

ADRA2A Tclin Alpha-2A adrenergic receptor 0 Activities

ADRB1 Tclin Beta-1 adrenergic receptor 0 Activities

ADRA1A Tclin Alpha-1A adrenergic receptor 0 Activities

AR Tclin Androgen receptor 0 Activities

MAOA Tclin Amine oxidase [flavin-containing] A 0 Activities

HTR2C Tclin 5-hydroxytryptamine receptor 2C 0 Activities

HTR1A Tclin 5-hydroxytryptamine receptor 1A 0 Activities

ADORA3 Tchem Adenosine receptor A3 0 Activities

HTR3A Tclin 5-hydroxytryptamine receptor 3A 0 Activities

HTR2B Tclin 5-hydroxytryptamine receptor 2B 0 Activities

EDNRA Tclin Endothelin-1 receptor 0 Activities

EDNRB Tclin Endothelin receptor type B 0 Activities

KCNH2 Tclin Potassium voltage-gated channel subfamily H member 2 0 Activities

OPRD1 Tclin Delta-type opioid receptor 0 Activities

OPRK1 Tclin Kappa-type opioid receptor 0 Activities

OPRM1 Tclin Mu-type opioid receptor 0 Activities

TACR1 Tclin Substance-P receptor 0 Activities

MLNR Tchem Motilin receptor 0 Activities

Names and Identifiers

Database links

Certificates

Certificate of Analysis(COA)

Related Documents

References

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