所有图片(1)
别名:
(2S)-1-[[(2r,3s)-5-氯-3-(2-氯苯基)-1-[(3,4-二甲氧基苯基)磺酰基]-2,3-二氢-3-羟基-1H-吲哚-2-基]羰基]-2-吡咯烷羧酰胺, SR49059
经验公式（希尔记法）:
C28H27Cl2N3O7S
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质量水平
检测方案
≥97% (HPLC)
形式
powder
旋光性
[α]/D -180 to -190°, c = 0.3 in chloroform-d
颜色
white to off-white
溶解性
DMSO: ≥10 mg/mL
创始人
Sanofi Aventis
储存温度
2-8°C
SMILES字符串
COc1ccc(cc1OC)S(=O)(=O)N2[C@@H](C(=O)N3CCC[C@H]3C(N)=O)[C@@](O)(c4ccccc4Cl)c5cc(Cl)ccc25
InChI
1S/C28H27Cl2N3O7S/c1-39-23-12-10-17(15-24(23)40-2)41(37,38)33-21-11-9-16(29)14-19(21)28(36,18-6-3-4-7-20(18)30)25(33)27(35)32-13-5-8-22(32)26(31)34/h3-4,6-7,9-12,14-15,22,25,36H,5,8,13H2,1-2H3,(H2,31,34)/t22-,25-,28+/m0/s1
InChI key
CEBYCSRFKCEUSW-NAYZPBBASA-N
基因信息
human ... AVPR1A(552) , OXTR(5021)
应用
SR 49059可用于精氨酸加压素（AVP）V1a受体介导的细胞信号转导研究中。
SR 49059已用于研究V1AR（1A型加压素受体）信号传导介导的 β肾上腺素能受体反应性及其对心力衰竭发展的影响。
生化/生理作用
SR 49059是一种有效的选择性精氨酸后叶加压素(AVP) V1a-受体拮抗剂。AVP是一种激素，在循环和水的稳态中发挥重要作用，并且在充血性心力衰竭（CHF）中对肾脏血流动力学改变、保水力和心脏重塑等具有重要作用。AVP受体有三种亚型，即V1a、V1b和V2。它们均属于大型视紫红质样G蛋白偶联受体家族。V(1a)拮抗剂可改善CHF中的水平衡和心脏肥大，可能有益于CHF中的保水力和心脏重塑。SR 49059在治疗雷诺氏病、痛经和安胎方面也显示出初步的积极结果。
特点和优势
该化合物由Sanofi Aventis开发。要浏览其他药物开发化合物和批准的药物/候选药物列表，单击此处。
WGK
nwg
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
Owen Jeffries et al.
Investigative ophthalmology & visual science, 51(3), 1591-1598 (2009-12-05)
To investigate the effects of arginine vasopressin (AVP) on Ca(2+) sparks and oscillations and on sarcoplasmic reticulum (SR) Ca(2+) content in retinal arteriolar myocytes. Fluo-4-loaded smooth muscle in intact segments of freshly isolated porcine retinal arteriole was imaged by confocal
Margareta Steinwall et al.
Gynecological endocrinology : the official journal of the International Society of Gynecological Endocrinology, 20(2), 104-109 (2005-04-13)
Relcovaptan (SR 49059) is a non-peptide, orally active vasopressin V1a receptor inhibitor. The effect on uterine contractions in 18 women with preterm labor in pregnancy weeks 32-36 was assessed in a double-blind investigation. The inclusion criterion was at least four
Véronique Perraudin et al.
The Journal of clinical endocrinology and metabolism, 91(4), 1566-1572 (2006-02-02)
Arginine vasopressin (AVP) stimulates steroid secretion from the normal human adrenal gland and some cortisol-producing adrenocortical tumors or hyperplasia through activation of the V(1a) receptor. The objective of the study was to investigate in vitro and in vivo the possible
Piotr Pierzynski
Reproductive biomedicine online, 22(1), 9-16 (2010-12-07)
Embryo transfer, the final stage of IVF/embryo transfer (IVF/ET) treatment, independently influences treatment outcome.Successful embryo implantation following embryo transfer, among other factors, is also dependant on uterine receptivity.Uterine contractile activity may adversely affect the implantation. Although increased contractions have been
R Lemmens-Gruber et al.
Cellular and molecular life sciences : CMLS, 63(15), 1766-1779 (2006-06-24)
Effects of vasopressin via V1a- and V2-receptors are closely implicated in a variety of water-retaining diseases and cardiovascular diseases, including heart failure, hyponatraemia, hypertension, renal diseases, syndrome of inappropriate antidiuretic hormone secretion, cirrhosis and ocular hypertension. As vasopressin receptors are
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