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THX-B

目录号 : GC67786

THX-B 是一种有效的、非多肽类型的 p75NTR (神经营养蛋白受体 p75) 拮抗剂。THX-B 可用于糖尿病、肾病、神经退行性和炎症性疾病的研究。

THX-B Chemical Structure

Cas No.:1372206-64-8

规格 价格 库存 购买数量
10 mM * 1mLinDMSO
¥594.00
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5mg
¥540.00
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10mg
¥900.00
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25mg
¥1,800.00
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50mg
¥2,880.00
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100mg
¥4,500.00
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Sample solution is provided at 25 µL, 10mM.

Description

THX-B is a potent and non-peptidic p75NTR (neurotrophin receptor p75) antagonist. THX-B can be used in the research of diabetic kidney disease, neurodegenerative and inflammatory disorders[1][2][3].

THX-B (10 μM, 4 days) decreases proliferation of myoblasts[1].
THX-B (10 μM, 1 h) inhibits NGF-induced phosphorylation of ERK1/2 in C2C12 myoblasts[1].
THX-B (20 μM, 24 h) decreases photoreceptor cell death and reactive gliosis in cultured rd10 retinas[2].

Western Blot Analysis[1]

Cell Line: C2C12 myoblasts
Concentration: 10 μM
Incubation Time: Pre-treated for 1 hour
Result: Inhibited βNGF-induced ERK2 phosphorylation by 67%.
Inhibited proNGF-induced ERK2 phosphorylation by 90%.

Immunofluorescence[1]

Cell Line: Cultured P22 rd10 retinas.
Concentration: 20 μM
Incubation Time: 24 h
Result: Attenuated the thickening and enlargement of processes of astrocytes and MÜller glia cells.

THX-B (50 μg in 125 μL PBS, i.p. weekly for 4 weeks) improves bladder function in a mouse model of diabetic voiding dysfunction[3].
THX-B (2 μL of 2 μg/μL, IVT injection, a single dose) elicits a neuroprotective effect on photoreceptor cells in P17 rd10 mice[2].
THX-B (40 μg in 20 μL, IVT injection) resolves the inflammatory, vascular, and neurodegenerative phases of the retinal pathology[4].

Animal Model: Mouse model of diabetic voiding dysfunction
Dosage: 50 μg in 125 μL PBS
Administration: Intraperitoneal injection (i.p.)
Result: Prevented bladder weight increase, which was 18% (95% CI 3%, 32%) and 37% (95% CI 14%, 60%) lower after 2 and 4 weeks of treatment.
Animal Model: P17 rd10 mice[1]
Dosage: 2 μL of 2 μg/μL, single dose
Administration: Intravitreal (IVT) injected in one eye
Result: Increased the number of photoreceptor rows as well as the ONL/INL ratio.
Decreased the total number of microglial cells in the treated retinas, as well as some of the inflammatory signs, such as GFAP, α2M and the proinflammatory cytokines IL-1β and TNFα.

[1]. Keren Ettinger, et al. Nerve growth factor stimulation of ERK1/2 phosphorylation requires both p75NTR and α9β1 integrin and confers myoprotection towards ischemia in C2C12 skeletal muscle cell model. Cell Signal. 2012 Dec;24(12):2378-88.
[2]. MarÍa PlatÓn-Corchado, et al. p75NTR antagonists attenuate photoreceptor cell loss in murine models of retinitis pigmentosa. Cell Death Dis. 2017 Jul 13;8(7):e2922.
[3]. Abubakr H Mossa, et al. Antagonism of proNGF or its receptor p75 NTR reverses remodelling and improves bladder function in a mouse model of diabetic voiding dysfunction. Diabetologia. 2020 Sep;63(9):1932-1946.
[4]. Alba Galan, et al. Subconjunctival Delivery of p75NTR Antagonists Reduces the Inflammatory, Vascular, and Neurodegenerative Pathologies of Diabetic Retinopathy. Invest Ophthalmol Vis Sci. 2017 Jun 1;58(7):2852-2862.

化学性质

Cas No. 1372206-64-8 SDF Download SDF
分子式 C16H24N6O4 分子量 364.4
溶解度 DMSO : 100 mg/mL (274.42 mM; Need ultrasonic) 储存条件 4°C, protect from light
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1 mM 2.7442 mL 13.7212 mL 27.4424 mL
5 mM 0.5488 mL 2.7442 mL 5.4885 mL
10 mM 0.2744 mL 1.3721 mL 2.7442 mL
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