2. TGF-beta/Smad Apoptosis Immunology/Inflammation Cytoskeleton
  3. TGF-β Receptor Apoptosis Interleukin Related Integrin Cadherin
  4. THR-123

THR-123 是一种口服有效的 ALK3 多肽激动剂。THR-123 与 ALK2 的结合相对较弱，但不与 ALK6 结合。THR-123 可抑制炎症、细胞凋亡 (apoptosis) 和上皮间质转化，并逆转五种急性和慢性肾损伤小鼠模型中已形成的纤维化。THR-123 可用于研究肾脏纤维化。

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Custom Peptide Synthesis

THR-123

THR-123 Chemical Structure

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Customer Review

THR-123 相关抗体

Top Publications Citing Use of Products

查看 TGF-β Receptor 亚型特异性产品:

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ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B

查看 Interleukin Related 亚型特异性产品:

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22

查看 Integrin 亚型特异性产品:

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αvβ1 αvβ3 αvβ5 αvβ6 αvβ8 α5β1 α1β1 α2β1 α4β1 α9β1 αIIbβ3 α4β7 αLβ2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

THR-123 is an orally active ALK3 peptide agonist. THR-123 has a relatively weak binding to ALK2, but does not bind to ALK6. THR-123 suppresses inflammation, apoptosis and the epithelial-to-mesenchymal transition program and reverses established fibrosis in five mouse models of acute and chronic renal injury. THR-123 can be used for the study of kidney fibrosis[1].

IC50 & Target[1]

BMPR1A

 

IL-6

 

IL-8

 

体外研究
(In Vitro)

THR-123 (0-100 μM，60 分钟) 以浓度依赖性方式抑制 TNF-α 诱导的 HK-2 细胞中 IL-6、IL-8 和 ICAM-1 的表达[1]。
THR-123 (250 μM) 显著抑制 TGF-β1、缺氧或顺铂诱导的 HK-2 细胞凋亡[1]。
THR-123 (10 μM) 可恢复被 TGF-β1 抑制的 E-钙粘蛋白表达，降低 CTGF 和 Snail1 的表达，并逆转细胞形态向间充质形式的转变[1]。

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

THR-123 相关抗体:
体内研究
(In Vivo)

THR-123 (5 mg/kg，口服，每日一次，持续 3 周) 可逆转肾毒性血清诱发的慢性肾纤维化 (NTN) 小鼠的肾纤维化[1]。 THR-123 (5 mg/kg，口服，每日一次，连续 7 天) 显著减少小鼠缺血再灌注损伤 (IRI) 模型中的肾小管坏死和组织损伤[1]。
THR-123 (5-15 mg/kg，口服或腹腔注射，每日一次，连续 5-7 天) 抑制小鼠单侧输尿管梗阻 (UUO) 模型中的间质体积扩张和胶原沉积[1]。
THR-123 (5 mg/kg，口服，每日一次，从 8 周龄到 16 周龄) 不会改变肾小球异常，并显著抑制COL4A3KO小鼠中观察到的肾小管萎缩和间质纤维化[1]。
THR-123 (5 mg/kg，口服，每日一次，持续 3 个月) 可抑制小鼠晚期糖尿病肾病相关的纤维化进展[1]。

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

Animal Model: Nephrotoxic serum nephritis, NTN model established in CD1 mice[1]
Dosage: 5 mg/kg
Administration: Oral administration (p.o.), once daily for 3 weeks
Result: Significantly reversed the already formed renal fibrosis, and improve glomerular sclerosis, renal tubular atrophy and interstitial fibrosis.
Significantly reduced renal function indicators.
Inhibited epithelial-mesenchymal transition (EMT) and reduce the number of E-cadherin and FSP1 double-positive renal tubular cells.
Reduced macrophage infiltration and activate the BMP-Smad signaling pathway (p-Smad1/5).
Animal Model: IRI model established in C57Bl/6 mice (8 weeks)[1]
Dosage: 5 mg/kg
Administration: Oral administration (p.o.), once daily for 7 days
Result: Significantly reduced the proportion of renal tubular necrosis and lowered the blood urea nitrogen level.
Reduced macrophage infiltration and alleviated cell apoptosis.
Animal Model: UUO model established in CD1 mice (8-12 week)[1]
Dosage: 5 and 15 mg/kg (p.o.) or 5 mg/kg (i.p.)
Administration: Oral administration (p.o.) or intraperitoneal injection (i.p.), once daily for 5-7 days
Result: Inhibited interstitial volume expansion and collagen deposition.
Reduced the expression of fibrosis markers (fibronectin and type I collagen).
Animal Model: Alport syndrome model established in eight weeks-old COL4A3KO mice on C57Bl/6 background[1]
Dosage: 5 mg/kg
Administration: Oral administration (p.o.), once daily from 8 weeks of age to 16 weeks of age
Result: Improved glomerular sclerosis, tubular damage and interstitial fibrosis.
Restored the expression of E-cadherin and reduce the fibroblast marker FSP1.
Animal Model: Streptozotocin (HY-13753) induced Diabetic nephropathy, DN model established in male CD1 mice (8 week)[1]
Dosage: 5 mg/kg
Administration: Oral administration (p.o.), once daily for 3 months
Result: Reduced mesangial matrix expansion, macrophage infiltration and cell apoptosis.
Delayed the deterioration of renal function in combination of Captopril (HY-B0368).
分子量

1926.13

Formula

C83H124N22O27S2
Sequence

Cys-Tyr-Phe-Asp-Asp-Ser-Ser-Asn-Val-Leu-Cys-Lys-Lys-Tyr-Arg-Ser (disulfide bridge: Cys1-Cys11)
Sequence Shortening

CYFDDSSNVLCKKYRS (disulfide bridge: Cys1-Cys11)
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.
纯度 & 产品资料
参考文献

THR-123 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

THR-123THR123THR 123TGF-β ReceptorApoptosisInterleukin RelatedIntegrinCadherinTransforming growth factor beta receptorsILRenal FibrosisBMP SignalingEpithelial-to-Mesenchymal Transition (EMT)RegenerationInhibitorinhibitorinhibit

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