Carbacyclin (Carbaprostacyclin)

A stable analog of PGI2

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货号: ajce49216
CAS: 69552-46-1
别名: Carbaprostacyclin; Carba-PGI2
分子式: C21H34O4
分子量: 350.49
纯度: >98%
溶解度: DMF: >10 mg/ml (from 6B-PGI2),DMSO: >5 mg/ml (from 6B-PGI2),Ethanol: >20 mg/ml (from 6B-PGI2),PBS pH 7.2: >80 μ g/ml (from 6B-PGI2)
储存: Store at -20°C
库存: 现货

Background

Carbaprostacyclin is a stable analog of PGI₂. When infused in rabbits or dogs, it inhibits ex vivo platelet aggregation, but the effect persists only 10 minutes after termination of the infusion. This implies rapid metabolic inactivation of carbaprostacyclin.¹ Carbaprostacyclin inhibits platelet aggregation with 10% of the molar potency exhibited by PGI₂.^1,2 The ED₅₀ of carbaprostacyclin for the in vitro inhibition of ADP-induced platelet aggregation in human PRP is 47 nM.³ It was also shown to effect terminal differentiation of preadipose into adipose cells and enhance the expression of angiotensinogen and adipose fatty acid binding protein with an EC₅₀ of about 0.5 ?M.⁴

1.Whittle, B.J.R., Moncada, S., Whiting, F., et al.Carbacyclin — a potent stable prostacyclin analogue for the inhibition of platelet aggregationProstaglandins19(4)605-627(1980) 2.Aiken, J.W., and Shebuski, R.J.Comparison in anesthetized dogs of the anti-aggregatory and hemodynamic effects of prostacyclin and a chemically stable prostacyclin analog, 6a-carba-PGI2 (carbacyclin)Prostaglandins19(4)629-643(1980) 3.Adaikan, P.G., Karim, S.M.M., and Lau, L.C.Platelet and other effects of carbaprostacyclin - a stable prostacyclin analogueProstaglandins Med.5(4)307-320(1980) 4.Aubert, J., Ailhaud, G., and Negrel, R.Evidence for a novel regulatory pathway activated by (carba)prostacyclin in preadipose and adipose cellsFEBS Lett.397(1)117-121(1996)

Protocol

Cell experiment:

Primary cultures of neonatal rat cardiomyocytes are prepared from the ventricles of 1-day-old Wistar rats, and are seeded at a density of 4 × 105/6-well plastic plates, 9 × 105/60 mm dishes, or 3 × 106/100 mm dishes with Dulbecco's modified Eagle's medium (DMEM) containing 10% fetal calf serum (FCS). After 40 h of incubation, cultured cardiomyocytes are serum-starved for 8 h before Carbacyclin stimulation.

Animal experiment:

Mice[3]Ten to twelve week-old male C57BL/6 mice (20-25 g) are used in the experiment. Mice (n = 4) are injected intraperitoneally with 100 μg of Carbacyclin, and are sacrificed at the times indicated. The hearts are excised, and the ventricles are then homogenized with 3 mL of Isogen for the following total RNA extraction procedure[3].

参考文献:

[1]. Takasuka M, et al. FTIR spectral study of intramolecular hydrogen bonding in thromboxane A2 receptor agonist (U-46619), prostaglandin (PG)E2, PGD2, PGF2 alpha, prostacyclin receptor agonist (carbacyclin), and their related compounds in dilute CCl4 solution: structure-activity relationships. J Med Chem. 1994 Jan 7;37(1):47-56.
[2]. Whittle BJ, et al. Carbacyclin--a potent stable prostacyclin analogue for the inhibition of platelet aggregation. Prostaglandins. 1980 Apr;19(4):605-27.
[3]. Kuroda T, et al. Carbacyclin induces carnitine palmitoyltransferase-1 in cardiomyocytes via peroxisome proliferator-activated receptor (PPAR) delta independent of the IP receptor signaling pathway. J Mol Cell Cardiol. 2007 Jul;43(1):54-62.