S5701
SR 49059
≥97% (HPLC), Arginine Vasopressin (AVP) V1a-receptor antagonist, powder
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
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关于此项目
经验公式（希尔记法）:
C28H27Cl2N3O7S
化学文摘社编号:
分子量:
620.50
UNSPSC Code:
51111800
PubChem Substance ID:
NACRES:
NA.77
MDL number:
产品名称
SR 49059, ≥97% (HPLC)
SMILES string
COc1ccc(cc1OC)S(=O)(=O)N2[C@@H](C(=O)N3CCC[C@H]3C(N)=O)[C@@](O)(c4ccccc4Cl)c5cc(Cl)ccc25
InChI key
CEBYCSRFKCEUSW-NAYZPBBASA-N
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
assay
≥97% (HPLC)
form
powder
optical activity
[α]/D -180 to -190°, c = 0.3 in chloroform-d
color
white to off-white
solubility
DMSO: ≥10 mg/mL
originator
Sanofi Aventis
storage temp.
2-8°C
Quality Level
Gene Information
human ... AVPR1A(552), OXTR(5021)
相关类别
Application
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。
Biochem/physiol Actions
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。
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。
Features and Benefits
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存储类别
11 - Combustible Solids
wgk
nwg
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
Atsuo Tahara et al.
European journal of pharmacology, 538(1-3), 32-38 (2006-05-09)
Mesangial cells are centrally-located glomerular pericytes with contractile, endocrine, and immunity-regulating functions. These cells are thought to maintain normal glomerular function, since mesangial cell proliferation and extracellular matrix formation are hallmarks of chronic glomerular disease. Vasopressin causes mesangial cell contraction
Anatol Manaenko et al.
Neurochemistry international, 58(4), 542-548 (2011-01-25)
Cerebral edema is a devastating consequence of brain injury leading to cerebral blood flow compromise and worsening parenchyma damage. In the present study, we investigated the effects of arginine-vasopressin (AVP) V(1a) receptor inhibition following an intracerebral hemorrhagic (ICH) brain injury
Daniela Braida et al.
Psychopharmacology, 220(2), 319-330 (2011-10-01)
Oxytocin (OT) and arginine-vasopressin (AVP) regulate social behavior in mammals. Zebrafish (Danio rerio) allows higher throughput and ease in studying human brain disorders. This study investigated in zebrafish the effect of non-mammalian homologs isotocin (IT) and vasotocin (AVT) in comparison
Andrea Kleindienst et al.
Acta neurochirurgica, 155(1), 151-164 (2012-11-29)
The hormone and neuropeptide arginine-vasopressin is designated to the maintenance of osmotic homoeostasis and blood pressure regulation. While experimental data show vasopressin V(1A) receptors to regulate aquaporin (AQP)4 water channel dependent brain water movement, the specific role in vasogenic and
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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