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| Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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≥99% for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
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SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
GPR81 agonist 1 is a potent and highly selective GPR81 agonist, with EC 50 s of 58 nM and 50 nM for human and mouse GPR81, respectively. GPR81 agonist 1 inhibits lipolysis in differentiated 3T3-L1 adipocytes. GPR81 agonist 1 suppresses lipolysis in mice without cutaneous flushing. GPR81 agonist 1 displays remarkable selectivity for GPR81 over GPR109a.
In Vitro
GPR81 agonist 1 (compound 2) (1-1000 nM) inhibits lipolysis in differentiated 3T3-L1 adipocytes. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
GPR81 agonist 1 (100 mg/kg; i.p.) suppresses lipolysis in mice without cutaneous flushing . GPR81 agonist 1 (10 mg/kg; i.p.) shows good bioavailability (71%) and C max (6.3 μM) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Nine-week-old male C57/Bl6 mice (fed and fasted mice) Dosage: 100 mg/kg Administration: I.p. Result: Reduced plasma FFA content of fed and fasted mice by approximately 50% and 35%, respectively, at 15 min postdose when intraperitoneally administered at a dose of 100 mg/kg. Animal Model: Male C57/Bl6 mice Dosage: 10 mg/kg (Pharmacokinetic Analysis) Administration: I.p.(Pharmacokinetic Analysis) Result: Showed good bioavailability (71%) and C max (6.3 μM).
Form:Solid
| Canonical Smiles | CC1CCC(CC1)C(=O)NC2=NC(=C(S2)CC(=O)N3CCN(CC3)C)C4=CC=CS4 |
|---|---|
| IUPAC Name | 4-methyl-N-[5-[2-(4-methylpiperazin-1-yl)-2-oxoethyl]-4-thiophen-2-yl-1,3-thiazol-2-yl]cyclohexane-1-carboxamide |
| InChIKey | ZLQAEANISSHOLB-UHFFFAOYSA-N |
| INCHI | 1S/C22H30N4O2S2/c1-15-5-7-16(8-6-15)21(28)24-22-23-20(17-4-3-13-29-17)18(30-22)14-19(27)26-11-9-25(2)10-12-26/h3-4,13,15-16H,5-12,14H2,1-2H3,(H,23,24,28) |
| Isomeric SMILES | CC1CCC(CC1)C(=O)NC2=NC(=C(S2)CC(=O)N3CCN(CC3)C)C4=CC=CS4 |
| PubChem CID | 86279608 |
| Molecular Weight | 446.63 |
Comprehensive hazard, handling, storage, and regulatory compliance document.
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View spec sheet →Taxonomy Tree
| Kingdom | Organic compounds |
|---|---|
| Superclass | Organoheterocyclic compounds |
| Class | Azoles |
| Subclass | Thiazoles |
| Intermediate Tree Nodes | Not available |
| Direct Parent | 2,4,5-trisubstituted thiazoles |
| Alternative Parents | N-arylamides N-methylpiperazines Thiophenes Tertiary carboxylic acid amides Heteroaromatic compounds Trialkylamines Secondary carboxylic acid amides Amino acids and derivatives Azacyclic compounds Organic oxides Hydrocarbon derivatives Carbonyl compounds |
| Molecular Framework | Aromatic heteromonocyclic compounds |
| Substituents | 2,4,5-trisubstituted 1,3-thiazole - N-arylamide - N-alkylpiperazine - N-methylpiperazine - 1,4-diazinane - Piperazine - Tertiary carboxylic acid amide - Heteroaromatic compound - Thiophene - Amino acid or derivatives - Carboxamide group - Secondary carboxylic acid amide - Tertiary amine - Tertiary aliphatic amine - Carboxylic acid derivative - Azacycle - Organic oxide - Organooxygen compound - Organonitrogen compound - Organic oxygen compound - Amine - Organic nitrogen compound - Hydrocarbon derivative - Carbonyl group - Aromatic heteromonocyclic compound |
| Description | This compound belongs to the class of organic compounds known as 2,4,5-trisubstituted thiazoles. These are compounds containing a thiazole ring substituted at positions 2, 4 and 5 only. |
| External Descriptors | Not available |
| Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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| Solubility | DMSO : 50 mg/mL (111.95 mM; Need ultrasonic) |
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