| Bioactivity | RQ-00203078 is a highly selective, potent and orally active TRPM8 antagonist with IC50s of 5.3 nM and 8.3 nM for rat and human TRPM8 channels, respectively. RQ-00203078 shows little inhibitory action against TRPV1, TRPA1, TRPV4, or TRPM2 channels[1][2]. | ||||||||||||
| Invitro | Intracellular Ca2+ imaging reveals that menthol induced both intracellular Ca2+ release and store-operated Ca2+ entry, with RQ-00203078 inhibiting each effect. RQ-00203078 (1-10 µM) inhibits HSC3 and HSC4 oral squamous carcinoma cell migration and invasion in vitro[2]. | ||||||||||||
| In Vivo | RQ-00203078 (compound 36) demonstrates excellent in vivo activity in a dose dependent manner with an ED50 value of 0.65 mg/kg in the Icilin-induced wet-dog shakes model in rats after oral administration[1].Excellent oral exposure of RQ-00203078 (compound 36) is confirmed independently in rat pharmacokinetics studies at 3 mg/kg (p.o.) administration, with a Cmax value of 2300 ng/mL and 86% bioavailability[1]. | ||||||||||||
| Name | RQ-00203078 | ||||||||||||
| CAS | 1254205-52-1 | ||||||||||||
| Formula | C21H13ClF6N2O5S | ||||||||||||
| Molar Mass | 554.85 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Masashi Ohmi, et al. Identification of a novel 2-pyridyl-benzensulfonamide derivative, RQ-00203078, as a selective and orally active TRPM8 antagonist. Bioorg Med Chem Lett. 2014 Dec 1;24(23):5364-8. [2]. Yoshihiko Okamoto, et al. Blockade of TRPM8 activity reduces the invasion potential of oral squamous carcinoma cell lines. Int J Oncol. 2012 May;40(5):1431-40. |
RQ-00203078
CAS: 1254205-52-1 F: C21H13ClF6N2O5S W: 554.85
RQ-00203078 is a highly selective, potent and orally active TRPM8 antagonist with IC50s of 5.3 nM and 8.3 nM for rat and
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