- RQ-00203078
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- $1.00 / 1KG
-
2019-12-31
- CAS:1254205-52-1
- Min. Order: 1KG
- Purity: Min98% HPLC
- Supply Ability: g/kg/ton
- RQ-00203078
-
- $1.00 / 1KG
-
2019-12-31
- CAS:1254205-52-1
- Min. Order: 1KG
- Purity: Min98% HPLC
- Supply Ability: g/kg/ton
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| | RQ-00203078 Basic information |
| Product Name: | RQ-00203078 | | Synonyms: | RQ-00203078;4-[[[3-Chloro-5-(trifluoromethyl)-2-pyridinyl][[4-(trifluoromethoxy)phenyl]methyl]amino]sulfonyl]benzoic acid;RQ-00203078;RQ 00203078;RQ00203078.;CS-1528;4-(N-(3-chloro-5-(trifluoromethyl)pyridin-2-yl)-N-(4-(trifluoromethoxy)benzyl)sulfamoyl)benzoic acid;Benzoic acid, 4-[[[3-chloro-5-(trifluoromethyl)-2-pyridinyl][[4-(trifluoromethoxy)phenyl]methyl]amino]sulfonyl]-;RQ-00203078 >=98% (HPLC);Transient receptor potential channels,Ca2+,TRPM8,RQ00203078,TRP Channel,migration,inhibit,Inhibitor,RQ 00203078,RQ-00203078,oral,invasion,menthol | | CAS: | 1254205-52-1 | | MF: | C21H13ClF6N2O5S | | MW: | 554.85 | | EINECS: | | | Product Categories: | Inhibitors | | Mol File: | 1254205-52-1.mol |  |
| | RQ-00203078 Chemical Properties |
| 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 |
| | RQ-00203078 Usage And Synthesis |
| 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. |
| | RQ-00203078 Preparation Products And Raw materials |
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