1. GPCR/G Protein Neuronal Signaling
  2. Cannabinoid Receptor
  3. LEI-101

LEI-101 是有效的、选择性的、具有口服活性的大麻素 CB2 受体的激动剂,其对 hCB2 的 pEC50 值为 8,对 hERG 的 pKi 值小于 4。LEI-101 与 CB2 受体的结合能力比 CB1 强100 倍。

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LEI-101 Chemical Structure

LEI-101 Chemical Structure

CAS No. : 2250025-91-1

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查看 Cannabinoid Receptor 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

LEI-101 is a potent, selective, and orally bioavailable cannabinoid CB2 receptor agonist, with a pEC50 of 8 for hCB2, and a pKi of less than 4 for hERG. LEI-101 is ~100-fold more potent in binding to CB2 receptors than to CB1 receptors[1][2].

体内研究
(In Vivo)

LEI-101 (2, 6, and 20 mg/kg, po) shows in vivo activity in a spinal nerve ligation model of neuropathic pain in rats[1].
LEI‐101 (p.o. or i.p.) at 3 or 10 mg/kg dose-dependently prevents kidney dysfunction and/or morphological damage induced by cisplatin in mice[2].

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

Animal Model: Neuropathy-induced mechanical allodynia in male wistar rats[1].
Dosage: 2, 6, and 20 mg/kg.
Administration: PO, single dose.
Result: Induced a dose-dependent antinociceptive effect after 2 h of dosing.
Animal Model: Fed male Wistar rats[1].
Dosage: 1 mg/kg iv and 5 mg/kg po (Pharmacological Analysis).
Administration: IV and PO.
Result: Exhibited T1/2 of 1.7 h and 0.8 h for po and iv administration.
Had a low clearance and 100% oral bioavailability.
分子量

508.99

Formula

C23H26ClFN4O4S

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
  • 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)
× = ×
C1   V1   C2   V2
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.

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产品名称:
LEI-101
目录号:
HY-124283A
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