RQ 00203078 is a potent TRPM8 antagonist (IC50 values are 5.3 and 8.3 nM for rat and human channels respectively). Exhibits >350-fold selectivity for TRPM8 over TRPV4, TRPV1 and TRPA1. Reduces HSC3 and HSC4 oral squamous carcinoma cell migration and invasion in vitro. Also attenuates icilin-induced wet dog shakes in rats. Orally active.
| Molecular Weight | 554.85 |
| Formula | C21H13ClF6N2O5S |
| CAS Number | 1254205-52-1 |
| Form | Solid |
| Solubility (25°C) | DMSO 55.48 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related TRP Channel Products |
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| N-Oleoyl glutamine
N-oleoyl-glutamine is a PM20D1-regulated N-acyl amino acids (NAAs). |
| N-Oleoyl valine
N-Oleoyl valine is a N-acyl valine compound that acts as a TRPV3 receptor antagonist. |
| TAT-M2NX
TAT-M2NX (tatM2NX) is a TRPM2 inhibitor with specific neuroprotective activity in male mice. |
| SOR-C13
SOR-C13, a carboxy-terminal truncated peptide, is a high-affinity TRPV6 antagonist with an IC50 value of 14 nM. |
| GsMTx4 TFA
GsMTx4 TFA is a spider venom peptide that selectively inhibits cation permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families. In addition, GsMTx4 TFA blocks cation-selective stretch-activated channels (SACs) and attenuates lysophosphatidylcholine (LPC)-induced astrocytotoxicity and microglial cell reactivity. |
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