Rolapitant hydrochloride hydrate (SCH619734 hydrochloride hydrate) is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant hydrochloride hydrate does not interact with CYP3A4. Rolapitant hydrochloride hydrate shows potent anti-emetic activity in a ferret emesis model.
| Molecular Weight | 554.95 |
| Formula | C25H29ClF6N2O3 |
| CAS Number | 914462-92-3 |
| Solubility (25°C) | DMSO ≥ 20 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 Neurokinin Receptor Products |
|---|
| Spantide II
Spantide II, an undecapeptide substance P (SP) analog, is a potent neurokinin-1 receptor (NK-1R) antagonist. |
| Substance P (7-11)
Substance P (7-11) is a C-terminal fragment of Substance P which can cause an increase in the intracellular calcium concentration. |
| [Sar9, Met(O2)11]-Substance P TFA
[Sar9,Met(O2)11]-Substance P TFA is a tachykinin NK1 receptor selective agonist. |
| [bAla8]-Neurokinin A(4-10)
[bAla8]-Neurokinin A(4-10) is a neurokinin 2 (NK2) receptor agonist. |
| [Sar9, Met(O2)11]-Substance P
[Sar9,Met(O2)11]-Substance P is a tachykinin NK1 receptor selective agonist. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
