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| | EST64454 Basic information |
| Product Name: | EST64454 | | Synonyms: | EST64454;EST64454 hydrochloride;EST64454 HCl;pain,Inhibitor,EST 64454,EST64454 hydrochloride,nerve,selective,EST-64454 hydrochloride,Sigma Receptor,EST-64454,oral,inhibit;EST64454 hydrochloride, 10 mM in DMSO | | CAS: | 1950569-11-5 | | MF: | C18H23ClF2N4O2 | | MW: | 400.85 | | EINECS: | | | Product Categories: | | | Mol File: | 1950569-11-5.mol |  |
| | EST64454 Chemical Properties |
| storage temp. | Store at -20°C | | solubility | DMSO : 100 mg/mL (249.47 mM; Need ultrasonic) | | form | Solid | | color | White to off-white |
| | EST64454 Usage And Synthesis |
| Uses | EST64454 hydrochloride is a selective and orally active sigma-1 receptor antagonist with a Ki of 22 nM. EST64454 hydrochloride has the potential for the research of the pain[1]. | | Biological Activity | EST64454 hydrochloride is a selective and orally active sigma-1 receptor antagonist with a Ki of 22 nM. EST64454 hydrochloride has the potential for the research of the pain[1].
EST64454 (10 mg/kg; p.o.; male Wistar rats) treatment shows the Cmax, t1/2, AUC0-∞, Vss and F% are 771 ng/mL, 3.4 hours, 1431 ng h/mL, 4.4 l/kg and 69%, respectively[1].EST64454 (10 mg/kg; p.o.; male CD1 mice) treatment shows the Cmax, t1/2, AUC0-∞, Vss and F% were 1178 ng/mL, <1 hours, 2645 ng h/mL, 1.2 l/kg and 60%, respectively[1]. | | in vivo | EST64454 (10 mg/kg; p.o.; male Wistar rats) treatment shows the Cmax, t1/2, AUC0-∞, Vss and F% are 771 ng/mL, 3.4 hours, 1431 ng h/mL, 4.4 l/kg and 69%, respectively[1].
EST64454 (10 mg/kg; p.o.; male CD1 mice) treatment shows the Cmax, t1/2, AUC0-∞, Vss and F% were 1178 ng/mL, <1 hours, 2645 ng h/mL, 1.2 l/kg and 60%, respectively[1]. | Animal Model: | Male Wistar rats (250-300 g)[1] | | Dosage: | 10 mg/kg | | Administration: | P.o. (Pharmacokinetic Analysis) | | Result: | The Cmax, t1/2, AUC0-∞, Vss and F% were 771 ng/mL, 3.4 hours, 1431 ng h/mL, 4.4 l/kg and 69%, respectively.
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| | References | [1]. Díaz JL, et al. EST64454: a Highly Soluble σ1 Receptor Antagonist Clinical Candidate for Pain Management. J Med Chem. 2020;63(23):14979-14988. |
| | EST64454 Preparation Products And Raw materials |
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