L-733060 hydrochloride

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L-733060 hydrochloride 

L-733060 hydrochloride 是一种有效的速激肽 NK1 受体拮抗剂。 L-733060 hydrochloride 以不会在啮齿动物中引起不良心血管影响的剂量抑制神经源性血浆外渗，同时还充当抗肿瘤剂。

L-733060 hydrochloride

L-733060 hydrochloride Chemical Structure

CAS No. : 148687-76-7

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生物活性

L-733060 hydrochloride is a potent tachykinin NK1 receptor antagonist. L-733060 hydrochloride inhibits neurogenic plasma extravasation at doses that do not cause adverse cardiovascular effects in rodents and also acts as an antitumoral agent[1][2].

IC50 & Target[1]

NK1

 

体外研究
(In Vitro)

L-733060 (30-300 nM) inhibits the [Ca2+]i mobilisation caused by substance P (100 nM) in a concentration-dependent manner in human tachykinin NK1 receptor-transfected CHO cells[1].
L-733060 (2.5-20 μM; 48 and or 96 h) results in a concentration-dependent cytotoxicity in COLO 858 cells[2].
L-733060 (10-30 μM; 24 and 48 h) inhibits MEL H0 cells proliferation with IC50s of 27.5 μM and 18.9 μM at 24 h and 48 h, respectively[2].
L-733060 (20-50 μM; and or 72 h) inhibits COLO 679 cells growth with IC50s of 33.8 μM and 31.5 μM at 30 h and 72 h, respectively[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[2]

Cell Line: COLO 858 cells
Concentration: 2.5, 5, 10, 20 μM
Incubation Time: 0, 48, 96 h
Result: Inhibited cells growth with IC50s of 8.7 μM and 7.1 μM at 48 h and 96 h, respectively.

体内研究
(In Vivo)

L-733060 (10-1000 μg/kg; i.v.) inhibits electrically stimulated plasma extravasation in dura mater of rats[1].
L-733060 (300-3000 μg/kg; i.v.) has no significant hypotensive or bradycardic effects are observed at doses of <3000 μg>[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague-Dawley rats (200 g) with electrical stimulation of the trigeminal ganglion[1]
Dosage: 10, 100, 1000 mg/kg
Administration: I.v. injection
Result: Produced a significant dose-related inhibition of plasma extravasation with an ID50 of 212±19 μg/kg.

分子量

439.82

Formula

C20H20ClF6NO
CAS 号

148687-76-7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Seabrook GR, et, al. L-733,060, a novel tachykinin NK1 receptor antagonist; effects in [Ca2+]i mobilisation, cardiovascular and dural extravasation assays. Eur J Pharmacol. 1996 Dec 12; 317(1):129-35.

    [2]. Muñoz M, et, al. Antitumoral action of the neurokinin-1 receptor antagonist L-733 060 on human melanoma cell lines. Melanoma Res. 2004 Jun;14(3):183-8.

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