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Olorinab

Catalog No. T14302 CAS 1268881-20-4

Synonyms: APD 371

Olorinab (APD 371) is a highly potent, selective and fully efficacious cannabinoid receptor type 2 (CB2) agonist. With an EC50 of 6.2 nM for hCB2.

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Olorinab, CAS 1268881-20-4

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Purity: 98%

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Description	Olorinab (APD 371) is a highly potent, selective and fully efficacious cannabinoid receptor type 2 (CB2) agonist. With an EC50 of 6.2 nM for hCB2.
Targets&IC50	hCB2:（EC50）6.2 nM
In vitro	A comprehensive in vitro profile of Olorinab (APD 371) (6) shows that single digit nanomolar potency and full intrinsic efficacy are maintained in all species assessed. Olorinab (APD 371) is highly selective for CB2 over CB1 in both binding and functional assays. Olorinab (APD 371) induces efficient receptor internalization (~106% relative to the CB1/2 agonist CP55,940) in CHO cells expressing HA-tagged rat CB2 suggesting that, according to the hypothesis, Olorinab (APD 371) would be able to drive agonist-induced receptor recycling[1].
In vivo	Olorinab (APD 371) significantly increases paw withdrawal thresholds at doses ≥3 mg/kg PO (ED50=2.3 mg/kg). The analgesic effects of Olorinab (APD 371) are shown to be highly likely mediated via activity at CB2 receptors[1]. In a separate experiment, a single dose of Olorinab (APD 371) (10 mg/kg, PO) inhibits paw withdrawal threshold for up to 4 hours after administration.

Synonyms	APD 371
Molecular Weight	357.41
Formula	C18H23N5O3
CAS No.	1268881-20-4

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Han S, et al. Discovery of APD371: Identification of a Highly Potent and Selective CB2 Agonist for the Treatment of Chronic Pain. ACS Med Chem Lett. 2017 Nov 30;8(12):1309-1313.

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Keywords

Olorinab 1268881-20-4 G蛋白偶联受体 Cannabinoid Receptor APD 371 Inhibitor inhibitor inhibit

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