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Evatanepag

SKU: orb1218402

Description

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.

Images & Validation

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Evatanepag

Key Properties

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CAS Number223488-57-1
MW468.57
Purity>98% (HPLC)
FormulaC25H28N2O5S
SMILESO=C(O)COC1=CC=CC(CN(CC2=CC=C(C(C)(C)C)C=C2)S(=O)(C3=CC=CN=C3)=O)=C1
TargetProstaglandin Receptor
SolubilityDMSO:32 mg/mL (68.29 mM)

Bioactivity

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In Vivo
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.
In Vitro
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.

Storage & Handling

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StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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CP-533536 free acid

Similar Products

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  • Evatanepag sodium [orb1739725]

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    C25H27N2NaO5S

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  • Evatanepag [orb1308320]

    99.68% (May vary between batches)

    223488-57-1

    468.57

    C25H28N2O5S

    1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 1 ml x 10 mM (in DMSO)
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Quick Database Links

Gene Symbol
Prostaglandin Receptor

Protocol Information

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5 mg
$ 320.00
10 mg
$ 500.00
25 mg
$ 830.00
50 mg
$ 1,190.00
100 mg
$ 1,670.00
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