| Identification | Back Directory | [Name]
RQ-00203078 | [CAS]
1254205-52-1 | [Synonyms]
CS-1528
RQ-00203078
RQ-00203078 >=98% (HPLC)
RQ-00203078;RQ 00203078;RQ00203078.
4-(N-(3-chloro-5-(trifluoromethyl)pyridin-2-yl)-N-(4-(trifluoromethoxy)benzyl)sulfamoyl)benzoic acid
4-[[[3-Chloro-5-(trifluoromethyl)-2-pyridinyl][[4-(trifluoromethoxy)phenyl]methyl]amino]sulfonyl]benzoic acid
Benzoic acid, 4-[[[3-chloro-5-(trifluoromethyl)-2-pyridinyl][[4-(trifluoromethoxy)phenyl]methyl]amino]sulfonyl]- | [Molecular Formula]
C21H13ClF6N2O5S | [MDL Number]
MFCD29049510 | [MOL File]
1254205-52-1.mol | [Molecular Weight]
554.85 |
| Chemical Properties | Back Directory | [Boiling point ]
602.0±65.0 °C(Predicted) | [density ]
1.588±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
insoluble in H2O; ≥18.85 mg/mL in DMSO; ≥27.25 mg/mL in EtOH | [form ]
solid | [pka]
3.39±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
RQ-00203078 is a selective antagonist of transient receptor potential melastatin 8 (TRPM8; IC50s = 8.3 and 5.8 nM in human and rat, respectively), while having little inhibitory action against TRPV1 (IC50 > 30 μM), TRPA1 (IC50 > 10 μM), TRPV4 (IC50 = 10 μM), or TRPM2 channels (IC50 > 10 μM). It attenuates icilin-induced wet-dog shakes in rats (ED50 = 0.65 mg/kg) after oral administration. RQ-00203078 has been shown to reduce HSC3 and HSC4 oral squamous carcinoma cell migration and invasion in vitro. TRPM8, a member of the TRP melastatin subgroup, plays a role in cold hyperalgesia and cold allodynia caused by disease conditions such as chemotherapy-induced peripheral neuropathy, diabetic neuropathy, migraine, and overactive bladder. It is also known to be involved in the tumor progression of certain carcinomas. | [Uses]
RQ 00203078 is a selective and orally active TRPM8 antagonist. | [in vitro]
in the menthol-induced calcium influx assay, rq-00203078 is a novel and highly potent trpm8 antagonist with human and rat ic50 values of 8.3 nm and 5.8 nm, respectively. rq-00203078 was highly selective over other trp channels [1]. | [in vivo]
rq-00203078 demonstrated excellent activity in vivo 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]. | [IC 50]
8.3 and 5.8 nm for htrpm8 and rtrpm8, respectively | [storage]
Store at +4°C | [References]
[1] ohmi m, shishido y, inoue t, ando k, fujiuchi a, yamada a, watanabe s, kawamura k. 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. |
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