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Pasireotide ditrifluoroacetate

CAS No. :

MCE 站：Pasireotide ditrifluoroacetate

产品活性：Pasireotide ditrifluoroacetate 是一种稳定的环六肽生长激素抑制素模拟物，与人 somatostatin receptor 具有很高的亲和性，包括 sst1/2/3/4/5，pK_i 值分别为 8.2/9.0/9.1/<7.0/9.9。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：Somatostatin Receptor

In Vitro: Pasireotide effectively inhibits the growth hormone releasing hormone (GHRH) induced growth hormone (GH) release in primary cultures of rat pituitary cells with an IC₅₀?of 0.4±0.1 nM.

In Vivo: Pasireotide potently suppressess GH secretion in rats. The ED₅₀?values determined at 1 and 6 h after injection of?pasireotide indicates its very long duration of action in vivo. In the rat,?pasireotide?strongly decreases IGF-1 plasma levels, with the efficacy being markedly enhanced compared with the effects elicited by?SMS 201-995?after 7 days of treatment. Furthermore, in rats, dogs, and rhesus monkeys, pasireotide potently and dose-dependently decreases IGF-1 levels for prolonged periods of time without desensitization. Pasireotide (160 mg/kg/month, s.c.) decreases serum insulin levels and increases serum glucose levels, reduces PNET tumor size, and demonstrates a reduction in tumor activity on PET/CT scan in Pdx1-Cre; Men1 floxed/floxed conditional knockout mice. Pasireotide (50 μg/kg) inhibits arthritic joint swelling in a dose-dependent manner, strongly inhibits joint swelling during the acute phase of AIA. Pasireotide- and octreotide-treated mice show significantly increased mechanical thresholds on the inflamed side. Pasireotide potently decreases secondary hyperalgesia to mechanical and thermal stimuli. Mechanical thresholds in the pasireotide-treated mice are significantly higher than those in the saline-treated or octreotide-treated animals.

相关产品：Drug Repurposing Compound Library Plus  |  FDA-Approved Drug Library Plus  |  Bioactive Compound Library Plus  |  Peptidomimetic Library  |  Macrocyclic Compound Library  |  Octreotide acetate  |  MK-4256  |  CYN 154806 TFA  |  Pasireotide L-aspartate salt  |  Cortistatin-14 TFA  |  L-803087  |  J-2156 TFA  |  CH 275  |  BIM-23056  |  Cyclosomatostatin  |  [Tyr1]-Somatostatin-14  |  SSTR5 antagonist 2

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