CarbaMiMidothioic acid, N,N'-dicyclohexyl-, (5,6-dihydro-6,6-diMethyliMidazo[2,1-b]thiazol-3-yl)Methyl ester, hydrochloride (1:2)
- Product Name
- CarbaMiMidothioic acid, N,N'-dicyclohexyl-, (5,6-dihydro-6,6-diMethyliMidazo[2,1-b]thiazol-3-yl)Methyl ester, hydrochloride (1:2)
- CAS No.
- 1092776-63-0
- Chemical Name
- CarbaMiMidothioic acid, N,N'-dicyclohexyl-, (5,6-dihydro-6,6-diMethyliMidazo[2,1-b]thiazol-3-yl)Methyl ester, hydrochloride (1:2)
- Synonyms
- IT1t dihydrochloride;IT1t (hydrochloride);IT1t dihydrochloride, 10 mM in DMSO;IT1t dihydrochloride,IT-1t dihydrochloride;N,N'-Dicyclohexylcarbamimidothioic acid (5,6-dihydro-6,6-dimethylimidazo[2,1-b]thiazol-3-yl)methyl ester dihydrochloride;CarbaMiMidothioic acid, N,N'-dicyclohexyl-, (5,6-dihydro-6,6-diMethyliMidazo[2,1-b]thiazol-3-yl)Methyl ester, hydrochloride (1;CarbaMiMidothioic acid, N,N'-dicyclohexyl-, (5,6-dihydro-6,6-diMethyliMidazo[2,1-b]thiazol-3-yl)Methyl ester, hydrochloride (1:2)
- CBNumber
- CB42705990
- Molecular Formula
- C21H35ClN4S2
- Formula Weight
- 443.11
- MOL File
- 1092776-63-0.mol
CarbaMiMidothioic acid, N,N'-dicyclohexyl-, (5,6-dihydro-6,6-diMethyliMidazo[2,1-b]thiazol-3-yl)Methyl ester, hydrochloride (1:2) Property
- Melting point:
- >187° (dec.)
- storage temp.
- Hygroscopic, -20°C Freezer, Under inert atmosphere
- solubility
- DMSO (Slightly), Methanol (Slightly)
- form
- Solid
- color
- White
N-Bromosuccinimide Price
- Product number
- 28434
- Product name
- IT1t (hydrochloride)
- Packaging
- 5mg
- Price
- $110
- Updated
- 2024/03/01
- Product number
- 28434
- Product name
- IT1t (hydrochloride)
- Packaging
- 25mg
- Price
- $459
- Updated
- 2024/03/01
- Product number
- 28434
- Product name
- IT1t (hydrochloride)
- Packaging
- 10mg
- Price
- $195
- Updated
- 2024/03/01
- Product number
- 4596
- Product name
- IT1tdihydrochloride
- Purity
- ≥99%(HPLC)
- Packaging
- 10
- Price
- $195
- Updated
- 2021/12/16
- Product number
- 4596
- Product name
- IT1tdihydrochloride
- Purity
- ≥99%(HPLC)
- Packaging
- 50
- Price
- $818
- Updated
- 2021/12/16
CarbaMiMidothioic acid, N,N'-dicyclohexyl-, (5,6-dihydro-6,6-diMethyliMidazo[2,1-b]thiazol-3-yl)Methyl ester, hydrochloride (1:2) Chemical Properties,Usage,Production
Description
IT1t is a chemokine (C-X-C motif) receptor 4 (CXCR4) antagonist (IC50s = 8 and 11 nM for the human and rat receptors, respectively). It is selective for CXCR4 over human ether-a-go-go-related gene potassium channels (hERG/Kv11.1; IC50 = 13,240 nM). IT1t inhibits calcium mobilization induced by chemokine (C-X-C-motif) ligand 12 (CXCL12) in CEM cells (IC50 = 1.1 nM) and decreases CXCL12-induced migration of Jurkat cells (IC50 = 79.1 nM). It inhibits replication of the HIV-1 strain NL4-3 in MT-4 cells and isolated human peripheral blood mononuclear cells (PBMCs) stimulated with phytohemagglutinin (PHA; IC50s = 14.2 and 19 nM, respectively). IT1t (20 μM) reduces tumor growth in an MDA-MB-231-B zebrafish xenograft model.
Uses
N,N''-Dicyclohexylcarbamimidothioic acid (5,6-dihydro-6,6-dimethylimidazo[2,1-b]thiazol-3-yl)methyl Ester Dihydrochloride is a potent CXCR4 antagonist. It also exhibits anti-viral activity against HIV.
in vivo
IT1t reduces the formation of TNBC early metastases in the zebrafish xenograft model. Tumor cell invasion at the metastatic site is effectively reduced upon CXCR4 silencing (Fig. 7B), similar to the antagonist IT1t [3].
IC 50
CXCL12/CXCR4: 2.1 nM (IC50); HIV-1 (X4): 14.2 nM (IC50, in MT-4 cells); HIV-1 (X4): 19 nM (IC50, in PBMCs)
storage
Store at +4°C
References
[1]. thoma g, streiff mb, kovarik j, et al. orally bioavailable isothioureas block function of the chemokine receptor cxcr4 in vitro and in vivo. j med chem, 2008, 51(24): 7915-7920.
CarbaMiMidothioic acid, N,N'-dicyclohexyl-, (5,6-dihydro-6,6-diMethyliMidazo[2,1-b]thiazol-3-yl)Methyl ester, hydrochloride (1:2) Preparation Products And Raw materials
Raw materials
Preparation Products
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