MR 409

MR 409;

MR 409 是一种选择性的生长激素释放激素 (GHRH) 激动剂。MR 409 通过增强脑缺血小鼠的内源性神经发生而具有显著的神经保护作用。MR 409 还可以抑制肺癌的体内生长。

MR 409amp;;

MR 409 Chemical Structure

CAS No. : 1445155-39-4

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生物活性

MR 409 is a selected growth hormone-releasing hormone (GHRH) agonist. MR 409 has remarkable neuroprotective effects through enhancing endogenous neurogenesis in cerebral ischemic mice. MR 409 also inhibits the in vivo growth of lung cancer[1][2][3][4].

体外研究
(In Vitro)

One week post-myocardial infarction (MI), MR 409 (MR-409) significantly reduces plasma levels of IL-2, IL-6, IL-10 and TNF-α compared to placebo[1].
MR 409 (MR-409; 1 μM) suppresses p53 expression in bovine pulmonary arterial endothelial cells (BPAECs)[2].
MR 409 (1 μM) induces the activation of JAK2, STAT3 and ERK1/2[2].
MR 409 (MR-409; 1 and 5 μM) decreases LPS-induced PGE2 and 8-iso-PGF levels, in a dose-dependent manner[3].
MR 409 (1 and 5μM) decreases LPS-induced lactate dehydrogenase (LDH) activity and nitrite production, without showing a dose-dependent effect[3].
MR 409 (1 and 5 μM) decreases LPS-induced gene expression of COX-2, NF-κB and iNOS in colon specimens, without a dose-dependent effect[3].
MR 409 (MR-409) can stimulate endogenous neurogenesis and improve the tMCAO-induced loss of neuroplasticity. MR 409 also enhances the proliferation and inhibits apoptosis of neural stem cells treated with oxygen and glucose deprivation-reperfusion[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[2]

Cell Line: BPAEC
Concentration: 1 μM
Incubation Time: 24, 48 and 72 hours
Result: Significantly suppressed p53 expression levels after 48 and 72 hours of treatment.

体内研究
(In Vivo)

MR 409 (MR-409) inhibits the in vivo growth of lung cancer xenografted into nude mice[3].
MR 409 (5 μg; s.c. treated daily for 4 weeks) reduces nociceptive response in mice[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Adult C57/BL6 male mice (5 weeks old, weight 20-22 g)[3]
Dosage: 5 µg
Administration: Treated daily by subcutaneous (s.c.) administration of 0.1 mL solution
Result: Showed maximal antinociceptive effects at 2 weeks. Sustained a moderate analgesic effect at 4 weeks.

分子量

3395.91

Formula

C153H252N44O43

CAS 号

1445155-39-4

Sequence Shortening

{N-Me}-Y-{D-Ala}-DAIFTNSYR-{Orn}-VL-{Abu}-QLSAR-{Orn}-LLQDI-{Nle}-DR-NHMe

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]. Rosemeire M Kanashiro-Takeuchi, et al. New therapeutic approach to heart failure due to myocardial infarction based on targeting growth hormone-releasing hormone receptor. Oncotarget. 2015;6(12):9728-39.

    [2]. Mohammad A Uddin, et al. GHRH antagonists support lung endothelial barrier function. Tissue Barriers. 2019;7(4):1669989.

    [3]. Lucia Recinella, et al. Protective effects of growth hormone-releasing hormone analogs in DSS-induced colitis in mice. Sci Rep. 2021 Jan 28;11(1):2530.

    [4]. Yueyang Liu, et al. Agonistic analog of growth hormone-releasing hormone promotes neurofunctional recovery and neural regeneration in ischemic stroke. Proc Natl Acad Sci U S A. 2021 Nov 23;118(47):e2109600118.

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