- Product Details
Keywords
- CEBRANOPADOL
- CEBRANOPADOL manufacturer/supplier
- 863513-91-1
Quick Details
- ProName: CEBRANOPADOL manufacturer/supplier
- CasNo: 863513-91-1
- Molecular Formula: C24H27FN2O
- Appearance: white or off-white powder
- Application: CEBRANOPADOL CAS: 863513-91-1 is us...
- DeliveryTime: in stock,shipment according to your re...
- PackAge: aluminum oil bag
- Port: shanghai
- ProductionCapacity: 1000 Metric Ton/Month
- Purity: 99%
- Storage: 0~20℃
- Transportation: by express,by sea, by air
- LimitNum: 1 Gram
- Related Substances: ≤1.0%
- Residue on Ignition: ≤0.1%
- Heavy Metal: ≤20ppm
- Valid Period: 2~3years
- Brand: Royall
- Grade Standard: Pharm grade
- Chemical Name: CEBRANOPADOL
- Molecular Weight: 378.48200
Superiority
We can provide GMP validation service that complies with SFDA, FDA, WHO and EU EMPA.Excellent registration team could help us easlily to register our products in different countries.If you and your customer are interested in some products or need CMO business service because of capacity limit, product cost limit or developing limit, plz feel free to contact us.
Besides, we could discuss the possible FDF distribution business. Hope to get the chance to discuss deeply.
Details
Hangzhou Jinlan Pharm-Drugs Technology Co., Limited is located in Hangzhou, Zhejiang Province. Neighboring Ningbo port, Shanghai port, Hangzhou Xiaoshan Int’l Airport and Shanghai Pudong Int’l Airport, the transportation and production environment are excellent.
We have established well market channels both domestically and overseas. Now JINLAN PHARMA is authorized by some Chinese chemical factories as universal agency and international area agency. Our products are exported to more than 100 countries and enjoy a well reputation, including Europe, USA, South America, India, south-east Asia and so on. Such as Canada, Germany, Spain, Australia, Russia, UAE, Estonia, Indonesia, Egypt, Pakistan and so on. Our machines with Excellent quality, Competitive price, Good after-service, are highly welcomed by our customers. We are pleased to know you and hope to be good friend and cooperator with you for our products. I am sure you will be satisfied with us.
Based on the philosophy of “Human-orient, Technical first, Quality product and High efficiency, Fact and Innovation”, JINLAN PHARMA highly welcome friends from all over the world to cooperate and get co-development.
Description
Cebranopadol (GRT-6005) is a novel opioid analgesic of the benzenoid class which is currently under development internationally by Grünenthal, a German pharmaceutical company, and its partner Depomed, a pharmaceutical company in the United States, for the treatment of a variety of different acute and chronic pain states. As of November 2014, it is in phase III clinical trials. Cebranopadol is unique in its mechanism of action as an opioid, binding to and activating all four of the opioid receptors; it acts as a full agonist of the nociceptin receptor (Ki = 0.9 nM; EC50 = 13.0; IA = 89%), μ-opioid receptor (Ki = 0.7 nM; EC50 = 1.2; IA = 104%), and δ-opioid receptor (Ki = 18 nM; EC50 = 110; IA = 105%), and as a partial agonist of the κ-opioid receptor (Ki = 2.6 nM; EC50 = 17; IA = 67%). The ED50 values of 0.5-5.6µg/kg when introduced IV & 25.1µg/kg after oral administration.
Cebranopadol shows highly potent and effective antinociceptive and antihypertensive effects in a variety of different animal models of pain. Notably, it has also been found to be more potent in models of chronic neuropathic pain than acute nociceptive pain compared to selective μ-opioid receptor agonists. Relative to morphine, tolerance to the analgesic effects of cebranopadol has been found to be delayed (26 days versus 11 days for complete tolerance). In addition, unlike morphine, cebranopadol has not been found to affect motor coordination or reduce respiration in animals at doses in or over the dosage range for analgesia. As such, it may have improved and prolonged efficaciousness and greater tolerability in comparison to currently available opioid analgesics.
As an agonist of the κ-opioid receptor, cebranopadol may have the capacity to produce psychotomimetic effects and other adverse reactions at sufficiently high doses, a property which could potentially limit its practical clinical dosage range.
Basic Info
Chemical Name |
6-fluoro-N,N-dimethyl-1'-phenylspiro[4,9-dihydro-3H-pyrano[3,4-b]indole-1,4'-cyclohexane]-1'-amine |
Synonyms |
Cebranopadol;Cebranopadol (USAN/INN);(1r,4r)-6'-fluoro-N,N-dimethyl-4-phenyl-4',9'-dihydro-3'H-spiro[cyclohexane-1,1'-pyrano[3,4-b]indol]-4-amine;(1r,4r)-6'-fluoro-N,N-dimethyl-4-phenyl-4',9'-dihydro-3'H-spiro[cyclohexane-1,1'-pyrano[3,4-b]indole]-4-amine; |
CAS No. |
863513-91-1 |
Molecular Formula |
C24H27FN2O |
Molecular Weight |
378.48200 |
PSA |
28.26000 |
LogP |
5.10610 |