2. GPCR/G Protein Neuronal Signaling
  3. Neurokinin Receptor
  4. Rolapitant hydrochloride hydrate

Rolapitant hydrochloride hydrate  (Synonyms: SCH619734 hydrochloride hydrate)

Cat. No.: HY-16436 Purity: 98.25%
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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.

For research use only. We do not sell to patients.

Rolapitant hydrochloride hydrate Chemical Structure

Rolapitant hydrochloride hydrate Chemical Structure

CAS No. : 914462-92-3

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Based on 1 publication(s) in Google Scholar

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Rolapitant hydrochloride hydrate Related Antibodies

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Description

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[1][2].

IC50 & Target[1]

human NK1

0.66 nM (Ki)

gerbil NK1

0.13 nM (Ki)

guinea pig NK1

0.72 nM (Ki)

monkey NK1

2.5 nM (Ki)

rabbit NK1

31.7 nM (Ki)

rat NK1

78.6 nM (Ki)

mouse NK1

60.4 nM (Ki)

In Vitro

Rolapitant hydrochloride hydrate has high selectivity over the human NK2 and NK3 subtypes of more than 1000-fold, as well as preferential affinity for human, guinea pig, gerbil and monkey NK1 receptors over rat, mouse and rabbit[1].
Rolapitant hydrochloride hydrate (1-1000 nM) inhibits the GR-73632 (an NK1 receptor agonist)-induced calcium efflux in a concentration-dependent and competitive manner in CHO cells expressing the human NK1 receptor[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Rolapitant hydrochloride hydrate Related Antibodies
In Vivo

Rolapitant hydrochloride hydrate (0.03-1 mg/kg for PO, 0.3-1 mg/kg for IV; single dosage) attenuates the GR-73632 (HY-P1192)-induced foot-tapping response in Mongolian Gerbils[1].
Rolapitant hydrochloride hydrate (0.03-1 mg/kg; PO; single dosage; observed for 72 h) blocks acute emesis induced by both apomorphine and cisplatin (HY-17394) in ferrets[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female Mongolian Gerbils (30-60 g; anesthetized by inhalation of an oxygen:isofluorane mixture after 4 h PO or immediately after IV, then injected with 5 μl of 3 pmol solution of GR-73632 via ICV)[1]
Dosage: 0.03, 0.1, 0.3 and 1 mg/kg for PO, 0.3 and 1 mg/kg for IV
Administration: PO or IV, single dosage
Result: Attenuated dose-dependently the GR-73632-induced foot-tapping response when administered PO 4 h before testing, with an ID90 of 0.3 mg/kg, and the inhibition in foot tapping for at least 24 h.
Blocked dose-dependently the foot tapping induced by GR-73632 when administered IV, with complete blockade observed at 1 mg/kg.
Animal Model: Ferrets (treated with subcutaneous administration of 0.125 mg/kg apomorphine or intraperitoneal administration of 10 mg/kg cisplatin)[1]
Dosage: 0.03, 0.1, 0.3 and 1 mg/kg
Administration: PO; single dosage; observed for 72 h
Result: Blocked dose-dependently acute emesis induced by both apomorphine and cisplatin in ferrets.
Produced a robust decrease in retches and vomits in ferrets that was maintained throughout the 72 h observation period.
Clinical Trial
Molecular Weight

554.95

Formula

C25H29ClF6N2O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1N[C@]2(CN[C@@](C3=CC=CC=C3)(CO[C@@H](C4=CC(C(F)(F)F)=CC(C(F)(F)F)=C4)C)CC2)CC1.[H]Cl.O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (450.49 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8020 mL 9.0098 mL 18.0196 mL
5 mM 0.3604 mL 1.8020 mL 3.6039 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8020 mL 9.0098 mL 18.0196 mL 45.0491 mL
5 mM 0.3604 mL 1.8020 mL 3.6039 mL 9.0098 mL
10 mM 0.1802 mL 0.9010 mL 1.8020 mL 4.5049 mL
15 mM 0.1201 mL 0.6007 mL 1.2013 mL 3.0033 mL
20 mM 0.0901 mL 0.4505 mL 0.9010 mL 2.2525 mL
25 mM 0.0721 mL 0.3604 mL 0.7208 mL 1.8020 mL
30 mM 0.0601 mL 0.3003 mL 0.6007 mL 1.5016 mL
40 mM 0.0450 mL 0.2252 mL 0.4505 mL 1.1262 mL
50 mM 0.0360 mL 0.1802 mL 0.3604 mL 0.9010 mL
60 mM 0.0300 mL 0.1502 mL 0.3003 mL 0.7508 mL
80 mM 0.0225 mL 0.1126 mL 0.2252 mL 0.5631 mL
100 mM 0.0180 mL 0.0901 mL 0.1802 mL 0.4505 mL
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Rolapitant hydrochloride hydrate Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Rolapitant hydrochloride914462-92-3SCH619734 hydrochlorideNeurokinin ReceptorNK receptorTachykinin receptorlong-actingorally activeanti-emeticemesisferretMongolian Gerbilsfoot tappingretchesvomitsInhibitorinhibitorinhibit

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