Valspodar - ≥98%, high purity , P-glycoprotein 1 inhibitor, CAS No.121584-18-7, P-glycoprotein 1 inhibitor

Item Number
V127307
Grouped product items
SKUSizeAvailabilityPrice Qty
V127307-1mg
1mg
In stock
$285.90
V127307-5mg
5mg
In stock
$999.90
V127307-10mg
10mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$1,599.90

Selective P-glycoprotein inhibitor

Basic Description

SynonymsSdz-psc-833 | SDZ PSC833 | Valspodar; (PSC-833 | SCHEMBL21751941 | Cyclosporin A, 6-[(2S,4R,6E)-4-methyl-2-(methylamino)-3-oxo-6-octenoic acid]-7-L-valine- | Sdz psc 833 | 6-[(2S,4R,6E)-4-Methyl-2-(methylamino)-3-oxo-6-octenoicacid]-7-L-valinecyclosporin
Specifications & PurityMoligand™, ≥98%
Biochemical and Physiological MechanismsValspodar is a P-glycoprotein (P-gp) inhibitor widely used in preclinical and clinical studies for overcoming multidrug resistance (MDR). In rat, Valspodar showed properties of low hepatic extraction and wide distribution, similar to that of its structura
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionP-glycoprotein 1 inhibitor
NoteWherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description

Valspodar (PSC 833) is a specific P-glycoprotein inhibitor and MDR regulator often used as a chemical sensitizer to study advanced epithelial ovarian cancer.

Product Properties

ALogP7.7

Associated Targets(Human)

ABCB1 Tchem Multidrug resistance protein 1 (0 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ABCG2 Tchem ATP-binding cassette sub-family G member 2 (4927 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ABCC2 Tchem Canalicular multispecific organic anion transporter 1 (1191 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SLCO1B1 Tchem Solute carrier organic anion transporter family member 1B1 (2672 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SLCO1B3 Tchem Solute carrier organic anion transporter family member 1B3 (2517 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SLCO1A2 Tchem Solute carrier organic anion transporter family member 1A2 (104 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SLCO2B1 Tchem Solute carrier organic anion transporter family member 2B1 (580 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ABCC4 Tchem Multidrug resistance-associated protein 4 (785 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MRP3 Multidrug resistance associated protein (78 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Abcc1 Multidrug resistance-associated protein 1 (42 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Abcb1b P-glycoprotein 1 (174 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Hdac6 Histone deacetylase 6 (222 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Abcb1a P-glycoprotein 3 (492 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
L929 (3802 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SARS-CoV-2 (38078 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

IUPAC Name (3S,6S,9S,12R,15S,18S,21S,24S,30S,33S)-1,4,7,10,12,15,19,25,28-nonamethyl-33-[(E,2R)-2-methylhex-4-enoyl]-6,9,18,24-tetrakis(2-methylpropyl)-3,21,30-tri(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecazacyclotritriacontane-2,5,8,11,14,17,20,23,26,29,32-undecone
INCHI InChI=1S/C63H111N11O12/c1-26-27-28-41(16)53(76)52-57(80)67-49(38(10)11)61(84)68(19)33-48(75)69(20)44(29-34(2)3)56(79)66-50(39(12)13)62(85)70(21)45(30-35(4)5)55(78)64-42(17)54(77)65-43(18)58(81)71(22)46(31-36(6)7)59(82)72(23)47(32-37(8)9)60(83)73(24)51(40(14)15)63(86)74(52)25/h26-27,34-47,49-52H,28-33H2,1-25H3,(H,64,78)(H,65,77)(H,66,79)(H,67,80)/b27-26+/t41-,42+,43-,44+,45+,46+,47+,49+,50+,51+,52+/m1/s1
InChi Key YJDYDFNKCBANTM-QCWCSKBGSA-N
Canonical SMILES CC=CCC(C)C(=O)C1C(=O)NC(C(=O)N(CC(=O)N(C(C(=O)NC(C(=O)N(C(C(=O)NC(C(=O)NC(C(=O)N(C(C(=O)N(C(C(=O)N(C(C(=O)N1C)C(C)C)C)CC(C)C)C)CC(C)C)C)C)C)CC(C)C)C)C(C)C)CC(C)C)C)C)C(C)C
Isomeric SMILES C/C=C/C[C@@H](C)C(=O)[C@H]1C(=O)N[C@H](C(=O)N(CC(=O)N([C@H](C(=O)N[C@H](C(=O)N([C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N([C@H](C(=O)N([C@H](C(=O)N([C@H](C(=O)N1C)C(C)C)C)CC(C)C)C)CC(C)C)C)C)C)CC(C)C)C)C(C)C)CC(C)C)C)C)C(C)C
WGK Germany 3
PubChem CID 5281884
Molecular Weight 1214.62

Certificates

Certificate of Analysis(COA)

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8 results found

Lot NumberCertificate TypeDateItem
L2215125Certificate of AnalysisSep 20, 2024 V127307
L2215742Certificate of AnalysisSep 20, 2024 V127307
D2424450Certificate of AnalysisApr 12, 2024 V127307
D2424451Certificate of AnalysisApr 12, 2024 V127307
D2424452Certificate of AnalysisApr 12, 2024 V127307
D2424453Certificate of AnalysisApr 12, 2024 V127307
L2410113Certificate of AnalysisApr 12, 2024 V127307
L2215123Certificate of AnalysisDec 02, 2022 V127307

Chemical and Physical Properties

SolubilityDMSO

Safety and Hazards(GHS)

WGK Germany 3

Related Documents

References

1. Loor F.  (1999)  Valspodar: current status and perspectives..  Expert Opin Investig Drugs,  (6): (807-35).  [PMID:15992133] [10.1021/op500134e]
2. Ellegaard AM et al..  (2016)  Repurposing Cationic Amphiphilic Antihistamines for Cancer Treatment..  EBioMedicine,  (130-9).  [PMID:27333030]

Solution Calculators