Veldoreotide

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Veldoreotide

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

252845-37-7

DG3173
PTR-3173

Veldoreotide (DG3173) 一种生长抑素类似物，可结合并激活生长抑素受体 (SSTR) 2/4/5。与 Octreotide (HY-P0036) 相比，Veldoreotide 在腺瘤中抑制生长激素分泌的比例更高。Veldoreotide 有被用作镇痛剂的潜力。

生物活性

Veldoreotide (DG3173) a somatostatin analogue, that can bind to and activate thesomatostatin receptors (SSTR) 2, 4, and 5. Veldoreotide inhibitsgrowth hormone (GH)secretion in adenomas compared withOctreotide(HY-P0036). Veldoreotide has the potential to be used as pain modulating agent^[1]

IC₅₀& Target^[1]

SSTR2

37.6 ± 4.5 nM (EC₅₀)

SSTR3

31.3 ± 14. nM (EC₅₀)

SSTR4

10.5 ± 3.4 nM (EC₅₀)

体外研究
(In Vitro)

Veldoreotide stimulates the SST2, SST4, and SST5 receptors with high potency and efficacy in the HEK293 cells, co-expressing these receptors with the GIRK2 channels; EC₅₀s of 37.6 ± 4.5 nM, 31.3 ± 14.4 nM and 10.5 ± 3.4 nM for GIRK2-SST2, GIRK2-SST4 and GIRK2-SST5, respectively^[1].
Veldoreotide (10 μM; 24 h) inhibits SST4-expressing BON-1 cells^[1].
Veldoreotide (DG3173) (100 nM or 1 μM; 6 h) inhibits GH secreation in adenomas with an IC₅₀of 0.49 nM^[2].

Cell Proliferation Assay^[1]

Cell Line:	SST4-expressing BON-1 cells
Concentration:	10 μM
Incubation Time:	24 h
Result:	Inhibited SST4-expressing BON-1 cells, while did not significantly inhibited wild type BON-1 cells.

Clinical Trial

分子量

1123.30

Formula

C₆₀H₇₄N₁₂O₁₀

CAS 号

252845-37-7

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.