Oliceridine HCl featured
WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#:510256
CAS#:1401031-39-7 (HCl)
Description:Oliceridine, also known as TRV130,is a µ- opioid receptor agonist, that is currently under evaluation in human clinical trials for the treatment of acute severe pain. It is a functionally selective μ-opioid receptor agonist developed by Trevena Inc. TRV130 elicits robust G protein signaling, with potency and efficacy similar to morphine, but with far less β-arrestin 2 recruitment and receptor internalization, it displays less adverse effects than morphine. (http://en.wikipedia.org/wiki/TRV130).
Price and Availability
Oliceridine HCl, purity > 98%, is in stock. The same day shipping out after order is received.
Chemical Structure
Theoretical Analysis
MedKoo Cat#: 510256Name: Oliceridine HCl CAS#: 1401031-39-7 (HCl)Chemical Formula: C22H30N2O2SExact Mass: 386.2028Molecular Weight: 386.5508Elemental Analysis: C, 68.36; H, 7.82; N, 7.25; O, 8.28; S, 8.30
Related CAS #:1401031-39-7 (HCl)1401028-24-7 (free base)
Synonym:TRV130; TRV 130; TRV130; Oliceridine; Oliceridine HCl; Oliceridine hydrochloride
IUPAC/Chemical Name:(R)-N-((3-methoxythiophen-2-yl)methyl)-2-(9-(pyridin-2-yl)-6-oxaspiro[4.5]decan-9-yl)ethanamine hydrochloride
InChi Key:YIIWXYLJZRISQP-ZMBIFBSDSA-N
InChi Code:InChI=1S/C22H30N2O2S.ClH/c1-25-18-7-15-27-19(18)16-23-13-10-21(20-6-2-5-12-24-20)11-14-26-22(17-21)8-3-4-9-22;/h2,5-7,12,15,23H,3-4,8-11,13-14,16-17H2,1H3;1H/t21-;/m1./s1
SMILES Code:COC1=C(CNCC[C@@](C2)(C3=NC=CC=C3)CCOC42CCCC4)SC=C1.[H]Cl
Technical Data
Additional Information
TRV130 is an opioid drug that is under evaluation in human clinical trials for the treatment of acute severe pain. It is a functionally selective μ-opioid receptor agonist developed by Trevena Inc. TRV130 elicits robust G protein signaling, with potency and efficacy similar to morphine, but with far less β-arrestin 2 recruitment and receptor internalization, it displays less adverse effects than morphine. (https://en.wikipedia.org/wiki/TRV130).
References
1: Soergel DG, Subach RA, Burnham N, Lark MW, JamesIE, Sadler BM, Skobieranda F, Violin JD, Webster LR. Biased agonism ofthe μ-opioid receptor by TRV130 increases analgesia and reduceson-target adverse effects versus morphine: A randomized, double-blind,placebo-controlled, crossover study in healthy volunteers. Pain. 2014Sep;155(9):1829-35. doi: 10.1016/j.pain.2014.06.011. Epub 2014 Jun 19.PubMed PMID: 24954166.
2: Violin JD, Crombie AL, Soergel DG, Lark MW. Biased ligands atG-protein-coupled receptors: promise and progress. Trends Pharmacol Sci.2014 Jul;35(7):308-16. doi: 10.1016/j.tips.2014.04.007. Epub 2014 May28. Review. PubMed PMID: 24878326.
3: Soergel DG, Subach RA, Sadler B, Connell J, Marion AS, Cowan CL,Violin JD, Lark MW. First clinical experience with TRV130:pharmacokinetics and pharmacodynamics in healthy volunteers. J ClinPharmacol. 2014 Mar;54(3):351-7. doi: 10.1002/jcph.207. Epub 2014 Jan28. PubMed PMID: 24122908.
4: Chen XT, Pitis P, Liu G, Yuan C, Gotchev D, Cowan CL, Rominger DH,Koblish M, Dewire SM, Crombie AL, Violin JD, Yamashita DS.Structure-activity relationships and discovery of a G protein biased μopioid receptor ligand,[(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain. JMed Chem. 2013 Oct 24;56(20):8019-31. doi: 10.1021/jm4010829. Epub 2013Oct 14. PubMed PMID: 24063433.
5: DeWire SM, Yamashita DS, Rominger DH, Liu G, Cowan CL, Graczyk TM,Chen XT, Pitis PM, Gotchev D, Yuan C, Koblish M, Lark MW, Violin JD. A Gprotein-biased ligand at the μ-opioid receptor is potently analgesicwith reduced gastrointestinal and respiratory dysfunction compared withmorphine. J Pharmacol Exp Ther. 2013 Mar;344(3):708-17. doi:10.1124/jpet.112.201616. Epub 2013 Jan 8. PubMed PMID: 23300227.
MedKoo，由化学家和药学家陈清奇博士。北卡罗莱纳州的研究三角区（ResearchTrianglePark,简称RTP)，是一家以研发、生产和销售小分子抗癌化合物为主的医药科技公司，该公司的业务范围主要是为全球所有从事抗癌药物研究和开发的制药公司，高校，研究院所，政府相关机构提供与抗癌药物分子相关的产品、试剂和技术服务。
中文名MedKoo中 文美帝药库医药科技公司创立于2008年总部位于美国东海岸
MedKoo是世界领先的供应商之一的抗癌化学试剂和激酶抑制剂。我们制造、销售和分发高质量的抗癌小分子肿瘤学研究试剂。我们的使命是建立世界上最全面的抗癌小分子的集合。我们也为医药行业提供高质量的研究服务、医学研究机构和学术机构。我们致力于提供优质的服务。 MedKoo是世界领先的供应商之一的抗癌化学试剂和激酶抑制剂。我们制造、销售和分发高质量的抗癌小分子肿瘤学研究试剂。我们的使命是建立世界上最全面的抗癌小分子的集合。我们也为医药行业提供高质量的研究服务、医学研究机构和学术机构。我们致力于提供优质的服务和分子有竞争力的价格。MedKoo是您可靠的合作伙伴采购药物发现和药物分子。 MedKoo是世界的抗癌化学试剂和激酶抑制剂供应商之一。我们制造，销售和分销用于肿瘤学研究的高质量抗癌小分子试剂。我们的使命是建立世界上全面的抗癌小分子集合。我们还为制药行业，医学研究组织和学术机构提供高质量的研究服务。我们致力于以具有竞争力的价格提供服务和分子。MedKoo是您可靠的药物发现和药物分子采购合作伙伴。 CRISPR-Cas9是近年兴起的用于靶向基因组特定位置，进行DNA修饰的重要工具。研究发现CRISPR是细菌为了应对病毒的攻击而演化而来的获得性免疫防御机制。具体来说，在CRISPR和Cas9的作用下，经由小RNA分子的引导，靶向并沉默入侵者遗传物质核酸的关键部分。在该系统中，crRNA（CRISPR-derivedRNA）与tracrRNA（trans-activatingRNA）结合形成的复合物能特异性识别靶基因序列，并引导Cas9核酸内切酶在靶定位点剪切双链DNA，随后，细胞的非同源末端连接修复机制（NHEJ）重新连接断裂处的基因组DNA，并引入插入或缺失突变。另外也可以提供一个外源双链供体DNA（Donor）通过同源重组（HR）整合进断裂处的基因组，从而达到对基因组DNA进行修饰的目的。
目前，CRISPR-Cas9系统的高效基因组编辑功能已被应用于多种生物，包括小鼠、大鼠、斑马鱼、秀丽隐杆线虫，也包含多种细菌和植物，甚至在人体上也有应用。
ebiomall.com
