Evatanepag

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Evatanepag 是一种 EP2 受体选择性前列腺素 E2 (PGE2) 激动剂，可诱导局部骨形成，EC50 为 0.3 nM。

Evatanepag is an EP2 receptor selective prostaglandin E2 (PGE2) agonist that induces local bone formation with EC50 of 0.3 nM.CP-533536 demonstrated the ability to heal fractures when administered locally as a single dose in rat models of fracture healing.

Evatanepag (10 nM, 30 min) inhibits hFcεRI-induced mast cells degranulation in a dose-dependent manner.Evatanepag (0.1 nM-10 μM, 12 min) results in an equivalent increase in intracellular cAMP in HEK-293 cells, with an IC50 of 50 nM.

Evatanepag (0.3-3.0 mg/kg, directly injected into the marrow cavity of the tibia) promotes bone formation in rats.Evatanepag (0.3, 3.0 mg/kg, intranasal administration, from day1 to day4) reduces HDM aeroallergen-induced increased RL response to methacholine in mice.Evatanepag (1 mg/kg, intravenous injection) demonstrates high i.v. clearance (Cl: 56 mL/min/kg) and a short half-life (t1/2: 0.33 h). Animal Model:Rats Dosage:0.3, 1.0, 3.0 mg/kg Administration:Directly injected into the marrow cavity of the tibia Result:Dose-dependently increased in bone area, bone mineral content, bone mineral density.Animal Model:HDM (house dust mite)-sensitized BALB/c mice Dosage:0.3 mg/kg, 3 mg/kg Administration:Intranasal administration, from day1 to day4.Result:Prevented aeroallergen-driven increased RL (lung resistance) at 0.3 mg/kg. Prevented the enhanced MC activity by approximately 48% at 3 mg/kg.

CP-533536 free acid

GPCR/G Protein

Prostaglandin Receptor

PGE2

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223488-57-1

468.57

C25H28N2O5S

>98% (HPLC)

DMSO:32 mg/mL (68.29 mM)

O=C(O)COC1=CC=CC(CN(CC2=CC=C(C(C)(C)C)C=C2)S(=O)(C3=CC=CN=C3)=O)=C1

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(-20℃)

With Ice Pack

≥ 2 years