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

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 MCHα1A 和 MCHD2 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。

在相同的摩尔浓度下，化合物盐形式与游离形式有相同的生物活性，但盐形式 SNAP 94847 hydrochloride 通常具有更好的水溶性和稳定性。

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SNAP 94847 Chemical Structure

SNAP 94847 Chemical Structure

CAS No. : 487051-12-7

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SNAP 94847 相关抗体

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MCE 顾客使用本产品发表的 2 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 IC50
230 nM
Compound: 16g, SNAP-94847
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
[PMID: 17668922]
体内研究
(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.
分子量

478.57

Formula

C29H32F2N2O2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

SNAP 94847 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SNAP 94847487051-12-7SNAP94847SNAP-94847MCHR1 (GPR24)Melanin concentrating hormone receptor 1AntidepressantanxiolyticanxietyInhibitorinhibitorinhibit

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