Grouped product items

SKU

Size

Availability

Price

Qty

A126902-250mg

250mg

Available within 4-8 weeks(?)

$1,629.90

A126902-1g

Available within 4-8 weeks(?)

$5,864.90

A126902-5g

In stock

$26,389.90

A126902-25g

25g

In stock

$118,754.90

Basic Description

Synonyms	Apremilast\|608141-41-9\|OTEZLA\|CC-10004\|CC 10004\|Apremilast (CC-10004)\|CC10004\|CHEBI:78540\|apremilastum\|UNII-UP7QBP99PN\|UP7QBP99PN\|(S)-N-(2-(1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl)-1,3-dioxoisoindolin-4-yl)acetamide\|HSDB 8221\|(S)-2-[1-(3-Etho
Specifications & Purity	Moligand™, ≥99%
Biochemical and Physiological Mechanisms	Apremilast, a novel small mol. inhibitor of PDE4. Apremilast has profound anti-inflammatory properties in animal models of inflammatory disease, as well as human chronic inflammatory diseases such as psoriasis and psoriatic arthritis. Apremilast blocks th
Storage Temp	Store at -20°C
Shipped In	Ice chest + Ice pads
Grade	Moligand™
Action Type	INHIBITOR
Mechanism of action	Phosphodiesterase 4 inhibitor
Note	5mg、25mg、100mg卖完停产，不再备货
Product Description	Apremilast (CC-10004) is a potent and orally active PDE4 and TNF-α inhibitor with IC50 of 74 nM and 77 nM, respectively. Apremilast(CC10004)是PDE4抑制剂，IC50为74 nM。

Product Properties

ALogP	1.8

Associated Targets

CTNNBIP1 Tbio Beta-catenin-interacting protein 1 0 Activities

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CYP1A2 Tchem Cytochrome P450 1A2 0 Activities

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CNR1 Tclin Cannabinoid receptor 1 0 Activities

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CYP2C19 Tchem Cytochrome P450 2C19 0 Activities

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DRD2 Tclin D(2) dopamine receptor 0 Activities

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CYP3A4 Tclin Cytochrome P450 3A4 0 Activities

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ESR1 Tclin Estrogen receptor 0 Activities

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ERBB2 Tclin Receptor tyrosine-protein kinase erbB-2 0 Activities

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

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NR3C1 Tclin Glucocorticoid receptor 0 Activities

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EGFR Tclin Epidermal growth factor receptor 0 Activities

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AVPR1A Tclin Vasopressin V1a receptor 0 Activities

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HDAC6 Tclin Histone deacetylase 6 0 Activities

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HRH1 Tclin Histamine H1 receptor 0 Activities

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SLC6A3 Tclin Sodium-dependent dopamine transporter 0 Activities

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SLC6A4 Tclin Sodium-dependent serotonin transporter 0 Activities

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PDE4D Tclin cAMP-specific 3',5'-cyclic phosphodiesterase 4D 6 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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PDE4C Tclin cAMP-specific 3',5'-cyclic phosphodiesterase 4C 1 Activities

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PTGS1 Tclin Prostaglandin G/H synthase 1 0 Activities

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PDE4B Tclin cAMP-specific 3',5'-cyclic phosphodiesterase 4B 4 Activities

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PTGS2 Tclin Prostaglandin G/H synthase 2 0 Activities

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

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DRD3 Tclin D(3) dopamine receptor 0 Activities

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KDR Tclin Vascular endothelial growth factor receptor 2 0 Activities

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CHRM3 Tclin Muscarinic acetylcholine receptor M3 0 Activities

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ADRA2B Tclin Alpha-2B adrenergic receptor 0 Activities

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CHRM2 Tclin Muscarinic acetylcholine receptor M2 0 Activities

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ADRA2C Tclin Alpha-2C adrenergic receptor 0 Activities

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HTR2A Tclin 5-hydroxytryptamine receptor 2A 0 Activities

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ADORA2A Tclin Adenosine receptor A2a 0 Activities

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ACHE Tclin Acetylcholinesterase 0 Activities

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ADRA2A Tclin Alpha-2A adrenergic receptor 0 Activities

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ADRB1 Tclin Beta-1 adrenergic receptor 0 Activities

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ADRA1A Tclin Alpha-1A adrenergic receptor 0 Activities

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AR Tclin Androgen receptor 0 Activities

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

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HTR2C Tclin 5-hydroxytryptamine receptor 2C 0 Activities

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ADORA1 Tclin Adenosine receptor A1 0 Activities

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HTR1A Tclin 5-hydroxytryptamine receptor 1A 0 Activities

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

ADORA3 Tchem Adenosine receptor A3 0 Activities

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

HTR3A Tclin 5-hydroxytryptamine receptor 3A 0 Activities

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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)

OPRD1 Tclin Delta-type opioid receptor 0 Activities

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

OPRM1 Tclin Mu-type opioid receptor 0 Activities

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MLNR Tchem Motilin receptor 0 Activities

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

Names and Identifiers

Pubchem Sid	488197590
Pubchem Sid Url	https://pubchem.ncbi.nlm.nih.gov/substance/488197590
IUPAC Name	N-[2-[(1S)-1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-1,3-dioxoisoindol-4-yl]acetamide
INCHI	InChI=1S/C22H24N2O7S/c1-5-31-19-11-14(9-10-18(19)30-3)17(12-32(4,28)29)24-21(26)15-7-6-8-16(23-13(2)25)20(15)22(24)27/h6-11,17H,5,12H2,1-4H3,(H,23,25)/t17-/m1/s1
InChi Key	IMOZEMNVLZVGJZ-QGZVFWFLSA-N
Canonical SMILES	CCOC1=C(C=CC(=C1)C(CS(=O)(=O)C)N2C(=O)C3=C(C2=O)C(=CC=C3)NC(=O)C)OC
Isomeric SMILES	CCOC1=C(C=CC(=C1)[C@@H](CS(=O)(=O)C)N2C(=O)C3=C(C2=O)C(=CC=C3)NC(=O)C)OC
Alternate CAS	608141-41-9
PubChem CID	11561674
MeSH Entry Terms	apremilast;CC 10004;CC-10004;CC10004;Otezla
Molecular Weight	460.5

Database links

ChEMBL Ligand	CHEMBL514800
PubChem CID	11561674
Wikipedia	Apremilast
CAS Registry No.	608141-41-9
PEP	apremilast
RCSB PDB Ligand	A9L
DrugCentral Ligand	4829
PubChem SID	488197590

Certificates

Certificate of Analysis(COA)

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13 results found

Lot Number	Certificate Type	Date	Item
G2215028	Certificate of Analysis	Apr 07, 2024	A126902
G2215029	Certificate of Analysis	Apr 07, 2024	A126902
E2113264	Certificate of Analysis	Feb 14, 2023	A126902
B2304154	Certificate of Analysis	Dec 14, 2022	A126902
B2304296	Certificate of Analysis	Dec 14, 2022	A126902
B2304297	Certificate of Analysis	Dec 14, 2022	A126902
B2102013	Certificate of Analysis	Dec 13, 2022	A126902
B2102015	Certificate of Analysis	Dec 13, 2022	A126902
B2102016	Certificate of Analysis	Dec 13, 2022	A126902
B2102017	Certificate of Analysis	Dec 13, 2022	A126902
B2102018	Certificate of Analysis	Dec 13, 2022	A126902
C2325025	Certificate of Analysis	Jun 06, 2022	A126902
C2325026	Certificate of Analysis	Jun 06, 2022	A126902

Chemical and Physical Properties

Solubility	DMSO 92 mg/mL Water <1 mg/mL Ethanol <1 mg/mL

Safety and Hazards(GHS)

Pictogram(s)	GHS08, GHS07
Signal	Danger
Hazard Statements	H302:Harmful if swallowed H312:Harmful in contact with skin H332:Harmful if inhaled H372:Causes damage to organs through prolonged or repeated exposure H360:May damage fertility or the unborn child H361:Suspected of damaging fertility or the unborn child H361fd:Suspected of damaging fertility; Suspected of damaging the unborn child H362:May cause harm to breast-fed children
Precautionary Statements	P261:Avoid breathing dust/fume/gas/mist/vapors/spray. P280:Wear protective gloves/protective clothing/eye protection/face protection. P302+P352:IF ON SKIN: wash with plenty of water. P321:Specific treatment (see ... on this label). P405:Store locked up. P501:Dispose of contents/container to ... P264:Wash hands [and …] thoroughly after handling. P260:Do not breathe dust/fume/gas/mist/vapors/spray. P271:Use only outdoors or in a well-ventilated area. P270:Do not eat, drink or smoke when using this product. P304+P340:IF INHALED: Remove person to fresh air and keep comfortable for breathing. P362+P364:Take off contaminated clothing and wash it before reuse. P330:Rinse mouth. P263:Avoid contact during pregnancy/while nursing. P203:Obtain, read and follow all safety instructions before use. P301+P317:IF SWALLOWED: Get medical help. P318:if exposed or concerned, get medical advice. P317:Get emergency medical help. P319:Get medical help if you feel unwell.

References

1. Man HW, Schafer P, Wong LM, Patterson RT, Corral LG, Raymon H, Blease K, Leisten J, Shirley MA, Tang Y et al.. (2009) Discovery of (S)-N-[2-[1-(3-ethoxy-4-methoxyphenyl)-2-methanesulfonylethyl]-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl] acetamide (apremilast), a potent and orally active phosphodiesterase 4 and tumor necrosis factor-alpha inhibitor.. J Med Chem, 52 (6): (1522-4). [PMID:19256507]
2. Schafer P. (2012) Apremilast mechanism of action and application to psoriasis and psoriatic arthritis.. Biochem Pharmacol, 83 (12): (1583-90). [PMID:22257911]
3. Gudjonsson JE, Johnston A, Ellis CN. (2012) Novel systemic drugs under investigation for the treatment of psoriasis.. J Am Acad Dermatol, 67 (1): (139-47). [PMID:22305044]
4. Schafer PH, Day RM. (2013) Novel systemic drugs for psoriasis: mechanism of action for apremilast, a specific inhibitor of PDE4.. J Am Acad Dermatol, 68 (6): (1041-2). [PMID:23680197]
5. Schafer PH, Parton A, Capone L, Cedzik D, Brady H, Evans JF, Man HW, Muller GW, Stirling DI, Chopra R. (2014) Apremilast is a selective PDE4 inhibitor with regulatory effects on innate immunity.. Cell Signal, 26 (9): (2016-29). [PMID:24882690]

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SKU	Size	Availability	Price
A126902-250mg	250mg	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$1,629.90
A126902-1g	1g	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$5,864.90
A126902-5g	5g	In stock	$26,389.90
A126902-25g	25g	In stock	$118,754.90

Apremilast - ≥99%, high purity , Phosphodiesterase 4 inhibitor, CAS No.608141-41-9, Phosphodiesterase 4 inhibitor