1. GPCR/G Protein
    Neuronal Signaling
  2. MCHR1 (GPR24)
  3. SNAP 94847

SNAP 94847 

目录号: HY-107625

SNAP 94847 是一种新型的,高亲和力的选择性黑色素浓缩激素受体 1 (MCHR1) 拮抗剂,其 (Ki= 2.2 nM, Kd=530 pM),它对 MCHα1AMCHD2 受体分别显示出 >80 倍和 >500 倍的选择性。 SNAP 94847 以高亲和力与小鼠和大鼠 MCHR1 结合,与其他 GPCR,离子通道,酶和转运蛋白的交叉反应性很小。

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SNAP 94847 Chemical Structure

SNAP 94847 Chemical Structure

CAS No. : 487051-12-7

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SNAP 94847 is a novel, high affinity selective melanin-concentrating hormonereceptor1 (MCHR1) antagonist with (Ki= 2.2 nM, Kd=530 pM), it displays >80-fold and >500-fold selectivity over MCHα1A and MCHD2 receptors respectively. SNAP 94847 binds with high affinity to the mouse and rat MCHR1 with minimal cross-reactivity to other GPCR, ion channels, enzymes, and transporters[1][3].

IC50 & Target

Ki: 2.2 nM (MCHR1); Kd: 530 pM (MCHR1)[1]

(In Vivo)

SNAP 94847 (oral gavage; 20 mg/kg; 14 days) shows an exaggerated locomotor response to acute quinpirole [treatment: F(2,19)=11.31, treatment × time: F(34,323) = 4.061], the effect of SNAP 94847 on quinpirole-evoked ambulations over the entire observation period is significant compared to the untreated animals[2].
SNAP 94847 (oral administration; 20 mg/kg; 21 days) in drink water, produces a significant increase in ambulation relative to untreated animals [treatment: F(3,28) = 8.971; treatment × time: F(51,476)=11.50]. shows a marked increase in locomotion is apparent after 40 min in the SNAP 94847-treated group,this effect is significant over 180 min[2].
SNAP 94847 (oral administration; 10 mg/kg), has a good bioavailability (59%), low plasma and blood clearances of 4.2 L/hr/kg and 3.3 L/hr/kg, respectively, and the half-life was shown to be 5.2 h in rats in a PK study[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Rat[2]
Dosage: 20 mg/kg
Administration: Oral administration; 20 mg/kg; 14 days
Result: Exhibited a exaggerated locomotor response to acute quinpirole.
Animal Model: Rat (PK study)[3]
Dosage: 10 mg/kg
Administration: oral gavage; 10 mg/kg
Result: Exhibited good physicochemical properties in rats.





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SNAP 94847