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NKH 477 Sale

(Synonyms: Colforsin dapropate hydrochloride) 目录号 : GC12640

NKH 477是一种新型水溶性毛喉素衍生物。

NKH 477 Chemical Structure

Cas No.:138605-00-2

规格 价格 库存 购买数量
1mg
¥263.00
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5mg
¥900.00
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10mg
¥1,620.00
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Sample solution is provided at 25 µL, 10mM.

Description

NKH 477 is a novel water-soluble forskolin derivative [1]. NKH 477 upregulates cAMP by activating adenylate cyclase, which is used to enhance myocardial contraction and dilate blood vessels [2]. NKH 477 is often used in the research and treatment of cardiovascular diseases such as heart failure [3-4].

In MCF7, HT29, A431, WiDr, RKO, A375, H630, Du145, SW480, and SW620 cells, NKH 477 (100μM; 48h) inhibits the proliferation of cancer cell lines [5]. In endothelial cells, NKH477 (0.1-1.0μM; 1h) increases cAMP in a concentration-dependent manner [2]. In CellSensorTM CRE-bla CHO-K1 cells, NKH 477 (30nM; 5h) induces CRE-conjugated β-lactamase activity in a concentration-dependent manner [6]. In endothelial cells, NKH477 (0.01-0.3μM; 1h) attenuated the phasic and the tonic increases in both [Ca2+]i and force induced by 10μM noradrenaline, in a concentration-dependent manner [7].

In specific pathogen-free Lewis rats and brown-norway rats, NKH 477 (1, 2, 3mg/kg; po; 10d) significantly prolonged allograft survival and reduced histopathological rejection in a dose-dependent manner [8]. In sprague-dawley rats, acute or chronic administration of NKH 477 (1.5mg/kg, ip, 9d) to rats significantly reduced their locomotion and upright behavior [9].

References:
[1]. Hosono M, Takahira T, Fujita A, et al. Cardiovascular and adenylate cyclase stimulant properties of NKH477, a novel water-soluble forskolin derivative. Journal of cardiovascular pharmacology. 1992 Apr 1; 19(4): 625-634.
[2]. Shafiq J, Suzuki S, Itoh T, Kuriyama H. Mechanisms of vasodilation induced by NKH477, a water-soluble forskolin derivative, in smooth muscle of the porcine coronary artery. Circulation research. 1992 Jul; 71(1): 70-81.
[3]. Fujita A, Takahira T, Hosono M, et al. Improvement of drug-induced cardiac failure by NKH477, a novel forskolin derivative, in the dog heart-lung preparation. The Japanese Journal of Pharmacology. 1992;58(4):375-381.
[4]. Hosoda S, Motomiya T, Katagiri T, et al. Acute Effect of NKH477, a Novel Forskolin Derivative, in Patients with Acute Heart Failure A Multicenter Placebo-Controlled Double-Blind Trial. Rinsho yakuri/Japanese Journal of Clinical Pharmacology and Therapeutics. 1997 Jun 30; 28(2): 583-602.
[5]. Faris Q. Alenzi, Mohamed L. Salem, Waleed G, et al. NKH477 inhibits proliferation and induces apoptosis in a panel of cancer cell lines. Journal of Personalized Medicine. 2010; 24(03): 182-187.
[6]. Xia M, Guo V, Huang R, et al. A cell-based β-lactamase reporter gene assay for the CREB signaling pathway. Current chemical genomics. 2009 Mar 17; 3: 7.
[7]. Ito S, Suzuki S, Itoh T. Effects of a water‐soluble forskolin derivative (NKH477) and a membrane‐permeable cyclic AMP analogue on noradrenaline‐induced Ca2+ mobilization in smooth muscle of rabbit mesenteric artery. British journal of pharmacology. 1993 Nov; 110(3): 1117-1125.
[8]. Nakashima S, Morikawa M, Komatsu K, et al. Antiproliferative effects of NKH477, a forskolin derivative, on cytokine profile in rat lung allografts. The Journal of heart and lung transplantation. 2005 Apr 1; 24(4): 462-469.
[9]. Kofman O, Bersudsky Y. Behavioural effects of NKH-477, a forskolin analogue, on locomotion and rearing in rats. International Journal of Neuropsychopharmacology. 2000 Mar 1; 3(1): 27-33.

NKH 477是一种新型水溶性毛喉素衍生物 [1]。NKH 477通过激活腺苷酸环化酶来上调cAMP水平,而腺苷酸环化酶具有增强心肌收缩和扩张血管的作用 [2]。NKH 477常用于研究和治疗心力衰竭等心血管疾病 [3-4]

在MCF7、HT29、A431、WiDr、RKO、A375、H630、Du145、SW480和SW620细胞中,NKH 477(100μM;48h)可抑制癌细胞系的增殖 [5]。在内皮细胞中,NKH477(0.1-1.0μM;1h)以浓度依赖性方式增加cAMP [2]。在CellSensorTM CRE-bla CHO-K1细胞中,NKH 477(30nM;5h)以浓度依赖性方式诱导CRE结合的β-内酰胺酶活性 [6]。在内皮细胞中,NKH477(0.01-0.3μM;1h)以浓度依赖性方式减弱10μM去甲肾上腺素引起的[Ca2+]i和力的阶段性和强直性增加 [7]

在无特定病原体的Lewis大鼠和Brown-Norway大鼠中,NKH 477(1、2、3mg/kg;po;10d)显著延长同种异体移植物的存活率,并以剂量依赖性方式减少组织病理学排斥反应 [8]。在Sprague-Dawley大鼠中,急性或慢性给予NKH 477(1.5mg/kg,ip,9d)显著降低其运动和直立行为 [9]

实验参考方法

Cell experiment [1]:

Cell lines

MCF7, HT29, A431, WiDr, RKO, A375, H630, Du145, SW480, and SW620 cells

Preparation Method

Cell culture media for the cell lines used in this study included: MCF7 (Fidler model cells); DMEM supplemented with 10% FBS and 1% L-glutamine for HT29, A431, WiDr, RKO, A375, H630, and Du145; and RPMI supplemented with 10% FBS and 1% L-glutamine for SW480 and SW620. All cells were routinely cultured in a humidified incubator at 37℃, 5% CO2, and subcultured before reaching confluence. Subculture of all adherent cells was performed by removing the culture medium, aspirating the monolayer, washing with PBS, and then washing with 10% trypsin/PE solution. After detachment, the cells were resuspended in the appropriate culture medium, counted, and transferred to tissue culture flasks or plates. Cells were typically treated with NKH 477 one day after plating.

Reaction Conditions

100μM; 48h

Applications

NKH 477 inhibits the proliferation of cancer cell lines.
Animal experiment [2]:

Animal models

Specific pathogen-free (SPF) Lewis rats and Brown-Norway (BN) rats

Preparation Method

Specific pathogen-free (SPF) Lewis rats (LEW) were used as recipients, and Brown-Norway rats (BN) or Lewis rats were used as donors. The recipient rats weighed 250-280g, and the donor rats weighed 220-250g. The experimental animals were randomly divided into five groups: syngeneic transplant group (LEW to LEW), untreated allogeneic transplant group (BN to LEW), and allogeneic transplant group treated with NKH 477 (doses of 1, 2, and 3mg/kg, respectively).

Dosage form

1, 2, 3mg/kg; po; 10d

Applications

NKH 477 significantly prolonged allograft survival and reduced histopathological rejection in a dose-dependent manner.

References:
[1]. Faris Q. Alenzi, Mohamed L. Salem, Waleed G, et al. NKH477 inhibits proliferation and induces apoptosis in a panel of cancer cell lines. Journal of Personalized Medicine. 2010; 24(03): 182-187.
[2]. Nakashima S, Morikawa M, Komatsu K, et al. Antiproliferative effects of NKH477, a forskolin derivative, on cytokine profile in rat lung allografts. The Journal of heart and lung transplantation. 2005 Apr 1; 24(4): 462-469.

化学性质

Cas No. 138605-00-2 SDF
别名 Colforsin dapropate hydrochloride
化学名 (3R,4aR,5S,6S,6aS,10S,10aR,10bS)-5-acetoxy-10,10b-dihydroxy-3,4a,7,7,10a-pentamethyl-1-oxo-3-vinyldodecahydro-1H-benzo[f]chromen-6-yl 3-(dimethylamino)propanoate hydrochloride
Canonical SMILES O[C@]1([C@]([C@H]2OC(C)=O)(C)O[C@@](C)(C=C)CC1=O)[C@]3(C)[C@@H]([C@@H]2OC(CCN(C)C)=O)C(C)(C)CC[C@@H]3O.Cl
分子式 C27H43NO8.HCl 分子量 546.1
溶解度 DMSO: ≥125 mg/mL;H2O : ≥ 20 mg/mL 储存条件 Store at -20°C,unstable in solution, ready to use.
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1 mM 1.8312 mL 9.1558 mL 18.3117 mL
5 mM 0.3662 mL 1.8312 mL 3.6623 mL
10 mM 0.1831 mL 0.9156 mL 1.8312 mL
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