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首页-小分子抑制剂&激动剂-GPCR-Cannabinoid Receptor-VIP36
VIP36

Chemical Structure : VIP36

CAS No.:

VIP36

货号: PC-24481Not For Human Use, Lab Use Only.

VIP36 is a potent, selective and highly peripherally restricted Gi-biased agonist of cannabinoid receptor type 1 (CB1) with Ki of 22 nM in radioligand competition assays, exerts analgesic efficacy through peripheral CB1 receptors and shows limited analgesic tolerance.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

VIP36 is a potent, selective and highly peripherally restricted Gi-biased agonist of cannabinoid receptor type 1 (CB1) with Ki of 22 nM in radioligand competition assays, exerts analgesic efficacy through peripheral CB1 receptors and shows limited analgesic tolerance.
VIP36 displayed significantly reduced β-arrestin-2 recruitment (Emax=47%) compared with MDMB-FUBINACA (FCU, Emax=178%).
VIP36 showspotent peripheral CB1 receptor-dependent analgesia with limited analgesic tolerance.
VIP36 shows no detectable recruitment of β-arrestin-1 to CB1.
VIP36 produces analgesia that is dependent on peripheral CB1 receptors, is more than 2,400-fold more peripherally restricted over the parent template (FUB) and about 13-fold more restricted than CB13.
VIP36 shows limited tolerance and does not engage central CB1 receptors.
VIP36 produced analgesic actions in mouse models of inflammatory, neuropathic and migraine pain.

物理化学性质&存储条件

分子量 526.61
分子式 C27H35FN6O4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

methyl (S)-2-(1-(4-fluorobenzyl)-6-(4-guanidinobutoxy)-1H-indazole-3-carboxamido)-3,3-dimethylbutanoate

参考文献

1. Rangari VA, et al. Nature. 2025 Mar 5. doi: 10.1038/s41586-025-08618-7.

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