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Rolapitant

Product Name
Rolapitant
CAS No.
552292-08-7
Chemical Name
Rolapitant
Synonyms
Roltant;SCH619734;Rolapitant;Rolapitant-d4;Rolapitant HCl;brand name: Varubi;Rolapitant USP/EP/BP;SCH619734 SCH-619734;Rolapitant(sch619734);rolapitant,914462-92-3
CBNumber
CB12628366
Molecular Formula
C25H26F6N2O2
Formula Weight
500.48
MOL File
552292-08-7.mol
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Rolapitant Property

Boiling point:
523.5±50.0 °C(Predicted)
Density 
1.34±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMF: 25 mg/ml; DMF:PBS(pH7.2) (1:2): 0.33 mg/ml; DMSO: 16 mg/ml; Ethanol: 3 mg/ml
pka
15.88±0.40(Predicted)
form 
Powder
color 
White to off-white
InChIKey
FIVSJYGQAIEMOC-ZGNKEGEESA-N
SMILES
N1[C@@]2(CC[C@@](CO[C@@H](C3=CC(C(F)(F)F)=CC(C(F)(F)F)=C3)C)(C3=CC=CC=C3)NC2)CCC1=O
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H361Suspected of damaging fertility or the unborn child

Precautionary statements

P201Obtain special instructions before use.

P202Do not handle until all safety precautions have been read and understood.

P281Use personal protective equipment as required.

P308+P313IF exposed or concerned: Get medical advice/attention.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical
Product number
23906
Product name
Rolapitant
Purity
≥98%
Packaging
1mg
Price
$32
Updated
2024/03/01
Cayman Chemical
Product number
23906
Product name
Rolapitant
Purity
≥98%
Packaging
5mg
Price
$116
Updated
2024/03/01
Cayman Chemical
Product number
23906
Product name
Rolapitant
Purity
≥98%
Packaging
10mg
Price
$214
Updated
2024/03/01
AK Scientific
Product number
3912BB
Product name
Rolapitant
Packaging
1mg
Price
$133
Updated
2021/12/16
ChemScene
Product number
CS-6387
Product name
Rolapitant
Purity
98.43%
Packaging
10mg
Price
$150
Updated
2021/12/16
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Rolapitant Chemical Properties,Usage,Production

Uses

Rolapitant (SCH619734) is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant does not interact with CYP3A4. Rolapitant shows potent anti-emetic activity in a ferret emesis model[1][2].

Definition

ChEBI: An azaspiro compound that is 1,7-diazaspiro[4.5]decan-2-one carrying additional phenyl and 1-{[3,5-bis(trifluoromethyl)phenyl]ethoxy}methyl substituents at position 8. Used (in the form of the hydrochloride hydrate) for the prevention of delayed nausea and vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy.

in vivo

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

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.

IC 50

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)

References

[1] Duffy RA, et al. Rolapitant (SCH 619734): a potent, selective and orally active neurokininNK1 receptor antagonist with centrally-mediated antiemetic effects inferrets. Pharmacol Biochem Behav. 2012 Jul;102(1):95-100. DOI:10.1016/j.pbb.2012.03.021
[2] Rapoport B, et al. Study of rolapitant, a novel, long-acting, NK-1 receptor antagonist, for the prevention of chemotherapy-induced nausea and vomiting (CINV) due to highly emetogenic chemotherapy (HEC). Support Care Cancer. 2015 Nov;23(11):3281-8. DOI:10.1007/s00520-015-2738-1

Rolapitant Preparation Products And Raw materials

Raw materials

Preparation Products

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Rolapitant Suppliers

China 132 India 2 United Kingdom 1 United States 9 Global 144
Wuhan Topule
Tel
+86-02787215551 +86-19945035818
Fax
027-87215551
Email
2936752263@qq.com
Country
China
ProdList
7986
Advantage
58
Hubei Kele Fine Chemical Co., Ltd
Tel
027-59101668 19945030958
Fax
027-59101668
Email
2881924765@qq.com
Country
China
ProdList
7938
Advantage
58
Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2922
Advantage
55
Chemvon Biotechnology Co., Ltd
Tel
021-50790412
Fax
+86-21-50790419
Email
info@chemvon.com
Country
China
ProdList
371
Advantage
57
Shanghai Topbiochem Technology Co., Ltd
Tel
021-58170097
Email
info@topbiochem.com
Country
China
ProdList
9510
Advantage
58
NCE Biomedical Co.,Ltd.
Tel
4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988
Fax
+86-27-87599188
Country
China
ProdList
1493
Advantage
55
Doly Chemical CO.,LTD.
Tel
021-34716221 15800796336
Fax
+86-21-31329566
Email
sales@dolypharm.com
Country
China
ProdList
289
Advantage
55
MedChemexpress LLC
Tel
021-58955995
Fax
609-228-5909
Email
sales@medchemexpress.cn
Country
United States
ProdList
4861
Advantage
58
Nanjing Sunlida Biological Technology Co., Ltd.
Tel
025-57798810
Fax
025-57019371
Email
sales@sunlidabio.com
Country
China
ProdList
3239
Advantage
55
TargetMol Chemicals Inc.
Tel
021-021-33632979 15002134094
Fax
021-33632979
Email
marketing@targetmol.com
Country
China
ProdList
7783
Advantage
58
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View Lastest Price from Rolapitant manufacturers

Shaanxi Xianhe Biotech Co., Ltd
Product
Rolapitant 552292-08-7
Price
US $0.00/kg
Min. Order
1kg
Purity
0.99
Supply Ability
1000kg
Release date
2025-04-30
BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.
Product
Rolapitant 552292-08-7
Price
US $0.00/g
Min. Order
1g
Purity
More Than 99%
Supply Ability
100kg/Month
Release date
2024-09-29
Wuhan Topule Biopharmaceutical Co., Ltd
Product
Rolapitant 552292-08-7
Price
US $8.00/g
Min. Order
1g
Purity
98%
Supply Ability
500g
Release date
2023-06-13

552292-08-7, RolapitantRelated Search:

ROLIPRAM Rolapitant (1R,2S,3R)-Isomer Rolapitant (1S,2R,3R)-Isomer Rolapitant (1S,2R,3S)-Isomer Rolapitant (1R,2R,3S)-Isomer ROLAPITANT HYDROCHLORIDE Rolapitant (1S,2S,3R)-Isomer Rolapitant (1S,2S,3S)-Isomer Rituximab Aprepitant Emtricitabine Tacrolimus Sumatriptan Memantine

  • Rolapitant
  • (5S,8S)-8-(((R)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)methyl)-8-phenyl-1,7-diazaspiro[4.5]decan-2-one hydrochloride.
  • Rolapitant HCl
  • Rolapitant(sch619734)
  • (5S,8S)-8-[[[(1R)-1-[3,5-Bis(trifluoromethyl)phenyl]ethyl]oxy]methyl]-8-phenyl-1,7-diazaspiro[4.5]decan-2-one
  • (5S,8S)-8-({(1R)-1-[3,5-Bis(trifluoromethyl)phenyl]ethoxy}methyl)-8-phenyl-1,7-diazaspiro[4.5]decan-2-one
  • rolapitant,914462-92-3
  • 1,7-Diazaspiro[4.5]decan-2-one,8-[[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]methyl]-8-phenyl-,(5S,8S)-
  • (5S,8S)-8-[[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]methyl]-8-phenyl-1,9-diazaspiro[4.5]decan-2-one
  • Rolapitant-d4
  • SCH619734
  • Rolapitant USP/EP/BP
  • Roltant
  • 3-Tritetradecanoylglycerol
  • brand name: Varubi
  • SCH619734 SCH-619734
  • foot tapping,long-acting,emesis,retches,Rolapitant,NK receptor,Neurokinin Receptor,vomits,SCH 619734,SCH-619734,anti-emetic,Inhibitor,inhibit,orally active,Mongolian Gerbils,Tachykinin receptor,ferret
  • (5S,8S)-8-(((R)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)methyl)-8-phenyl-1,7-diazaspiro[4.5]decan-2-one
  • Rolapitant, 10 mM in DMSO
  • 552292-08-7
  • C25H26F6N2O2