Description
ATC0175 hydrochloride is a potent, selective and orally active antagonist of melanin-concentrating hormone receptor 1 (MCH1) with IC50 of 13 nM for MCH1. It was also shown to have affinity for 5-HT2B and 5-HT1A receptors with IC50 of 9.66 nM and 16.9 nM respectively. Melanin-concentrating hormone receptor (MCH1), a member of the G protein-coupled receptor family 1, is an integral plasma membrane protein which binds melanin-concentrating hormone. The protein can inhibit cAMP accumulation and stimulate intracellular calcium flux, and is probably involved in the neuronal regulation of food consumption. In vitro, assays showed that this compound is a potent antagonist with a high affinity for MCH1R. The receptor binding and the functional assay (MCH-induced increase in [Ca2+]) indicated that ATC0175 is a noncompetitive antagonist at MCH1Rs 1. In vivo, ATC0175 displayed anxiolytic effects in numerous animal models of anxiety including the social interaction test, elevated plus-maze test, maternal separation-induced vocalization and stress-induced hyperthermia. In addition, ATC0175 treatment also exhibited antidepressant effects in the forced swimming test 2.
Product information
CAS Number: 510733-97-8
Molecular Weight: 461.94
Formula: C23H26ClF2N5O
Chemical Name: 3,4-difluoro-N-[(1s,4s)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl]benzamide hydrochloride
Smiles: Cl.CN(C)C1=NC(N[C@H]2CC[C@H](CC2)NC(=O)C2C=C(F)C(F)=CC=2)=NC2=CC=CC=C21
InChiKey: HUUPKFUYSQNNLO-FAESNJTISA-N
InChi: InChI=1S/C23H25F2N5O.ClH/c1-30(2)21-17-5-3-4-6-20(17)28-23(29-21)27-16-10-8-15(9-11-16)26-22(31)14-7-12-18(24)19(25)13-14;/h3-7,12-13,15-16H,8-11H2,1-2H3,(H,26,31)(H,27,28,29);1H/t15-,16+;
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
Products are for research use only. Not for human use.
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