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My CartCAS：610309-89-2
Storage：Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：Solid
Qty：
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| CAS | 610309-89-2 |
| Name | Carvedilol Phosphate |
| Molecular Formula | C24H26N2O4·H3PO4·1/2H2O |
| Molecular Weight | 513.48 |
| Solubility | Soluble in DMSO(Need ultrasonic) |
| Purity | ≥98% |
| Appearance | Solid |
| Storage | Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| SMILES | COC1=CC=CC=C1OCCNCC(COC2=CC=CC3=C2C4=CC=CC=C4N3)O.COC1=CC=CC=C1OCCNCC(COC2=CC=CC3=C2C4=CC=CC=C4N3)O.O.OP(=O)(O)O.OP(=O)(O)O |
| InChIKey | LHNYXTULDSJZRB-UHFFFAOYSA-N |
| InChI | InChI=1S/2C24H26N2O4.2H3O4P.H2O/c2*1-28-21-10-4-5-11-22(21)29-14-13-25-15-17(27)16-30-23-12-6-9-20-24(23)18-7-2-3-8-19(18)26-20;2*1-5(2，3)4;/h2*2-12，17，25-27H，13-16H2，1H3;2*(H3，1，2，3，4);1H2 |
| PubChem CID | 11954344 |
| Target Point | Adrenergic Receptor |
| Passage | Endocrinology & Hormones;GPCR & G Protein；Neuronal Signaling |
| Background | It is a non-selective beta /α-1 receptor blocker. It is also an inducer of autophagy and can inhibit NLRP3 inflammasome. |
| Biological Activity | Carvedilol Phosphate 是一种非选择性β/α-1 阻滞剂。可抑制脂质过氧化反应，IC50 为 5 μM。是一种多效降压药，可用于治疗心绞痛和充血性心力衰竭。是一种自噬诱导剂，可抑制 NLRP3 炎性体。[1-3] |
| IC50 | lipid peroxidation: 5μM(IC50)[1] |
| In Vitro | Carvedilol inhibited lipid peroxidation in a dose-dependent manner with a 50% inhibitory concentration(IC50)of 5 mumol/l. Moreover，superoxide generation by activated human neutrophils in vitro was also inhibited by carvedilol with an IC50 of 28 mumol/l. Finally，carvedilol was shown to scavenge oxygen free radicals in a cell-free system with an IC50 of 25 mumol/l.[1] Carvedilol(CVL)attenuated NLRP3 inflammasome activation and pyroptosis in mouse macrophages，without affecting activation of the AIM2，NLRC4 and non-canonical inflammasomes. CVL caused autophagic induction through a Sirt1-dependent pathway，which inhibited the NLRP3 inflammasome.[2] In the in vivo mouse model of NLRP3-associated peritonitis，oral administration of CVL reduced peritoneal recruitment of neutrophils; the levels of IL-1β，IL-18，active caspase-1，ASC，IL-6，TNF-α，MCP-1，and CXCL1 in the lavage fluids; and the levels of NLRP3 and HO-1 in the peritoneal cells.[3] |
| In Vivo | After oral administration of one capsule of 25 mg or 50 mg carvedilol，significant reductions in the systolic and diastolic blood pressures(p less than 0.05-0.001)were observed in patients all had essential hypertension. Cardiac output showed a small，non-significant decrease from 5.81/min to 5.1 l/min.[1] In the rats of acute myocardial infarction，carvedilol(1 mg/kg，intravenously)reduced the infarct size by 47%(P < 0.01). In the minipigs the infarct size was reduced by 46 and 89%(P < 0.01)with carvedilol(0.3 or 1 mg/kg intravenously). In dogs with permanent coronary occlusion，carvedilol produced dose-dependent reductions in the infarct size of 46 and 63% for 0.3 and 1 mg/kg，respectively(P < 0.05).[2] |
| Data Literature Source | [1]. Eggertsen R，et al. Acute haemodynamic effects of carvedilol (BM 14190)，a new combined beta-adrenoceptor blocker and precapillary vasodilating agent，in hypertensive patients. Eur J Clin Pharmacol. 1984;27(1):19-22. [2]. Feuerstein GZ，et al. Myocardial protection by the novel vasodilating beta-blocker，carvedilol: potential relevance of anti-oxidant activity. J Hypertens Suppl. 1993 Jun;11(4):S41-8. [3]. Wong WT，et al. Repositioning of the β-Blocker Carvedilol as a Novel Autophagy Inducer That Inhibits the NLRP3 Inflammasome. Front Immunol. 2018 Aug 22;9:1920. |
| Unit | Bottle |
| Specification | 25mg 50mg |
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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