RQ-00203078 Struktur

RQ-00203078

Bezeichnung:RQ-00203078

CAS-Nr1254205-52-1

Englisch Name:RQ-00203078

CBNumberCB93040792

SummenformelC21H13ClF6N2O5S

Molgewicht554.85

MOL-Datei1254205-52-1.mol

RQ-00203078 physikalisch-chemischer Eigenschaften

Siedepunkt	602.0±65.0 °C(Predicted)
Dichte	1.588±0.06 g/cm3(Predicted)
storage temp.	Store at -20°C
Löslichkeit	insoluble in H2O; ≥18.85 mg/mL in DMSO; ≥27.25 mg/mL in EtOH
Aggregatzustand	solid
pka	3.39±0.10(Predicted)
Farbe	White to off-white

Gefahreninformationscode (GHS)

RQ-00203078 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
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.
Verwenden
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
Lager
Store at +4°C
Einzelnachweise
[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 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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