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MedKoo Cat#: 463097 | Name: TJ-M2010-5
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

TJ-M2010-5 is a Tie2 receptor inhibitor, which targets the Tie2 receptor (also known as angiopoietin-1 receptor). The Tie2 receptor plays a crucial role in angiogenesis (the formation of new blood vessels) and maintaining the integrity of blood vessels, and it is particularly involved in regulating endothelial cell function and vascular stability. By inhibiting Tie2 signaling, TJ-M2010-5 aims to disrupt the growth of abnormal blood vessels, which is a key feature in diseases like cancer and diabetic retinopathy.

Chemical Structure

TJ-M2010-5
CAS#1357471-57-8 (free base)

Theoretical Analysis

MedKoo Cat#: 463097

Name: TJ-M2010-5

CAS#: 1357471-57-8 (free base)

Chemical Formula: C23H26N4OS

Exact Mass: 406.1827

Molecular Weight: 406.55

Elemental Analysis: C, 67.95; H, 6.45; N, 13.78; O, 3.94; S, 7.89

Price and Availability

Size Price Availability Quantity
5mg USD 350.00 2 Weeks
10mg USD 550.00 2 Weeks
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Related CAS #
1357471-57-8 (free base) 2459882-83-6 (HCl)
Synonym
TJ-M2010-5; TJM2010-5; TJ M2010-5; TJ-M20105; TJ-M2010 5; TJM20105; TJ M2010 5;
IUPAC/Chemical Name
3-(4-benzylpiperazin-1-yl)-N-(4-phenylthiazol-2-yl)propanamide
InChi Key
DTIQJBUDKQVBLT-UHFFFAOYSA-N
InChi Code
InChI=1S/C23H26N4OS/c28-22(25-23-24-21(18-29-23)20-9-5-2-6-10-20)11-12-26-13-15-27(16-14-26)17-19-7-3-1-4-8-19/h1-10,18H,11-17H2,(H,24,25,28)
SMILES Code
[H]C1=CC=CC(CN(CC2)CCN2CCC(NC3=NC(C4=CC([H])=C([H])C=C4)=CS3)=O)=C1
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 406.55 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Zou Z, Du D, Miao Y, Yang Y, Xie Y, Li Z, Zhou L, Zhang L, Zhou P, Jiang F. TJ-M2010-5, a novel MyD88 inhibitor, corrects R848-induced lupus-like immune disorders of B cells in vitro. Int Immunopharmacol. 2020 Aug;85:106648. doi: 10.1016/j.intimp.2020.106648. Epub 2020 Jun 5. PMID: 32504998. 2: Liu J, Zhang X, Wang H, Zhang M, Peng Y, Li M, Xie L, Jiang F, Gong Y, Zhao Q, Zhou P. Implication of myeloid differentiation factor 88 inhibitor TJ-M2010-5 for therapeutic intervention of hepatocellular carcinoma. Hepatol Res. 2019 Oct;49(10):1182-1194. doi: 10.1111/hepr.13359. Epub 2019 May 9. PMID: 31074165. 3: Ding Z, Du D, Yang Y, Yang M, Miao Y, Zou Z, Zhang X, Li Z, Zhang X, Zhang L, Wang X, Zhao Y, Jiang J, Jiang F, Zhou P. Short-term use of MyD88 inhibitor TJ-M2010-5 prevents d-galactosamine/lipopolysaccharide-induced acute liver injury in mice. Int Immunopharmacol. 2019 Feb;67:356-365. doi: 10.1016/j.intimp.2018.11.051. Epub 2018 Dec 21. PMID: 30583234. 4: Xing S, Zhang X, Huang X, Xie L, Jiang F, Zhou P. Modulating the conformation of the TIR domain by a neoteric MyD88 inhibitor leads to the separation of GVHD from GVT. Leuk Lymphoma. 2019 Jun;60(6):1528-1539. doi: 10.1080/10428194.2018.1537487. Epub 2018 Dec 3. PMID: 30501537. 5: Yang M, Chen G, Zhang X, Ding Z, Miao Y, Yang Y, Chen ZK, Jiang F, Chang S, Zhou P. A novel MyD88 inhibitor attenuates allograft rejection after heterotopic tracheal transplantation in mice. Transpl Immunol. 2019 Apr;53:1-6. doi: 10.1016/j.trim.2018.11.006. Epub 2018 Nov 22. PMID: 30472390. 6: Liu JH, He L, Zou ZM, Ding ZC, Zhang X, Wang H, Zhou P, Xie L, Xing S, Yi CZ. A Novel Inhibitor of Homodimerization Targeting MyD88 Ameliorates Renal Interstitial Fibrosis by Counteracting TGF-β1-Induced EMT in Vivo and in Vitro. Kidney Blood Press Res. 2018;43(5):1677-1687. doi: 10.1159/000494745. Epub 2018 Oct 31. PMID: 30380557. 7: Li C, Zhang LM, Zhang X, Huang X, Liu Y, Li MQ, Xing S, Yang T, Xie L, Jiang FC, Jiang HY, He WT, Zhou P. Short-term Pharmacological Inhibition of MyD88 Homodimerization by a Novel Inhibitor Promotes Robust Allograft Tolerance in Mouse Cardiac and Skin Transplantation. Transplantation. 2017 Feb;101(2):284-293. doi: 10.1097/TP.0000000000001471. PMID: 27607533. 8: Zhang X, Xing S, Li M, Zhang L, Xie L, He W, Liu J, Chang S, Jiang F, Zhou P. Beyond knockout: A novel homodimerization-targeting MyD88 inhibitor prevents and cures type 1 diabetes in NOD mice. Metabolism. 2016 Sep;65(9):1267-77. doi: 10.1016/j.metabol.2016.05.005. Epub 2016 May 14. PMID: 27506734. 9: Xie L, Jiang FC, Zhang LM, He WT, Liu JH, Li MQ, Zhang X, Xing S, Guo H, Zhou P. Targeting of MyD88 Homodimerization by Novel Synthetic Inhibitor TJ-M2010-5 in Preventing Colitis-Associated Colorectal Cancer. J Natl Cancer Inst. 2015 Dec 28;108(4):djv364. doi: 10.1093/jnci/djv364. PMID: 26712311.