343248-86-2
343248-86-2 structure
- Name: ERA63
- Chemical Name: ERA63
- CAS Number: 343248-86-2
- Molecular Formula:
- Molecular Weight: 310.47
- Catalog: Research Areas Inflammation/Immunology
- Create Date: 2018-06-21 15:43:34
- Modify Date: 2025-08-21 08:33:10
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ERA63 is a selective estrogen receptor α agonist.
| Name | ERA63 |
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| Description | ERA63 is a selective estrogen receptor α agonist. |
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| Related Catalog | |
| In Vivo | The pharmacologic properties for the ERα agonist ERA-63 (Org 37663) have been shown efficacy in inflammatory models at 1.5 mg/kg. ERA-63 dose-dependently decreases the TT-specific response whereas treatment with the ERβ-agonist ERB-79 has no effect on TT-specific swelling. ERA-63 inhibits the tetanus toxoid (TT)-specific DTH response in WT and ERβ-/- mice but not in ERα-/- mice. ERA-63 inhibits the tetanus-specific delayed type hypersensitivity response in WT and ERβKO but not in the ERαKO mice. Therapeutic administration of the selective agonist ERA-63 decreases the clinical signs of arthritis dose-dependently. In addition, the AUC analysis over the 20-day treatment period reveals a significant dose-dependent reduction in the ERA-63-treated mice when compared with vehicle control[1]. After 28 days of treatment with dosages ranging from pharmacological up to clearly toxic levels, selected ERA-63 dose levels (0.167–0.2, 1.67–2 and 16.7–20 mg/kg) are expected to have comparable estrogenic activity to respective EE dose levels (0.05, 0.5 and 5 mg/kg)[2]. |
| Animal Admin | Mice: WT C57bl/6 (n=8 per group) mice are ovariectomized and treated once daily orally with the selective ERα agonist ERA-63 (6 mg/kg), EE (0.025, 0.25 and 2.5 mg/kg) or vehicle (0.5% gelatin- 5% mannitol in water) only from day -1 to day 9. The selective ERβ agonist ERB-79 (3 mg/kg) is administered subcutaneously and compared with vehicle (subcutaneous). Further DTH validation experiments are performed with ERα - and ERβ-deficient mice. The ERβKO mice are generated in-house and fully characterized. ERαKO, ERβKO and WT are ovariectomized and treated once daily orally with the selective ERα agonist ERA-63 (6 mg/kg) or vehicle (0.5% gelatin and 5% mannitol in water) from day -1 to day 9. The DTH response is assessed[1]. |
| References |
| Molecular Weight | 310.47 |
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