An MC1R antagonist
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ATC 0175

Item No. 42376

Technical Information
Formal Name
N-[cis-4-[[4-(dimethylamino)-2-quinazolinyl]amino]cyclohexyl]-3,4-difluoro-benzamide, monohydrochloride
CAS Number
510733-97-8
Molecular Formula
C23H25F2N5O • HCl
Formula Weight
Purity
≥95%
Formulation
A solid
DMSO: Slightly soluble: 0.1-1 mg/mLEthanol: Slightly soluble: 0.1-1 mg/mL
SMILES
O=C(C1=CC(F)=C(C=C1)F)N[C@@H](CC2)CC[C@@H]2NC(N=C3N(C)C)=NC4=C3C=CC=C4.Cl
InChi Code
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+;
InChi Key
HUUPKFUYSQNNLO-FAESNJTISA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    ATC 0175 is a melanocortin receptor 1 (MC1R) antagonist (IC50 = 7.23 nM).1 It is selective for MC1R over MC2R (IC50 = >10,000 nM) but does antagonize the serotonin (5-HT) receptor subtypes 5-HT2B and 5-HT1A (IC50s = 9.66 and 16.9 nM, respectively). ATC 0175 (3 nM) inhibits [35S]GTPγS binding and calcium influx induced by melanin-concentrating hormone (MCH; Item No. 24462) in HEK293 cells expressing human MC1R. In vivo, ATC 0175 (1, 3, and 10 mg/kg) reduces stress-induced decreases in the time spent in the open arms of the elevated plus maze in mice. It also decreases immobility time in the forced swim test in mice.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Chaki, S., Yamaguchi, J.-i., Yamada, H., et alATC0175: An orally active melanin-concentrating hormone receptor 1 antagonist for the potential treatment of depression and anxiety. CNS Drug Rev. 11(4), 341-152 (2005).