Rolapitant (SCH619734) is an orally bioavailable, centrally-acting, selective neurokinin 1 receptor (NK1-receptor) antagonist with a Ki of 0.66 nM. Upon oral administration, rolapitant competitively binds to and blocks the activity of the NK1-receptor in the central nervous system, thereby inhibiting the binding of the endogenous ligand, substance P (SP). Rolapitant is active at 0.1 and 1 mg/kg in both acute and delayed emesis models in ferrets, respectively.
Molecular Weight | 500.48 |
Formula | C25H26F6N2O2 |
CAS Number | 552292-08-7 |
Solubility (25°C) | DMSO ≥ 25 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.
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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. |
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