ChemicalBook > CAS DataBase List > NBI-74330

NBI-74330

Product Name
NBI-74330
CAS No.
855527-92-3
Chemical Name
NBI-74330
Synonyms
NBI-74330;N-[(1R)-1-[3-(4-Ethoxyphenyl)-3,4-dihydro-4-oxopyrido[2,3-d]pyrimidin-2-yl]ethyl]-4-fluoro-N-(3-pyridinylmethyl)-3-(trifluoromethyl)benzeneacetamide;N-{1-[3-(4-ethoxyphenyl)-4-oxo-3,4-dihydropyrido[2,3-d]pyrimidin- 2-yl]ethyl}-2-[4-fluoro-3-(trifluoromethyl)phenyl]-n-(3-pyridinyl Methyl)acetamide;(R)-N-(1-(3-(4-Ethoxyphenyl)-4-oxo-3,4-dihydropyrido[2,3-d]pyrimidin-2-yl)ethyl)-2-(4-fluoro-3-(trifluoromethyl)phenyl)-N-(pyridin-3-ylmethyl)acetamide;Benzeneacetamide, N-[(1R)-1-[3-(4-ethoxyphenyl)-3,4-dihydro-4-oxopyrido[2,3-d]pyrimidin-2-yl]ethyl]-4-fluoro-N-(3-pyridinylmethyl)-3-(trifluoromethyl)-
CBNumber
CB62628189
Molecular Formula
C32H27F4N5O3
Formula Weight
605.58
MOL File
855527-92-3.mol
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NBI-74330 Property

Boiling point:
752.5±70.0 °C(Predicted)
Density 
1.32±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMSO:100.0(Max Conc. mg/mL);165.1(Max Conc. mM)
pka
4+-.0.11(Predicted)
form 
Powder
color 
Light yellow to yellow
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

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N-Bromosuccinimide Price

Cayman Chemical
Product number
28442
Product name
NBI 74330
Packaging
1mg
Price
$359
Updated
2024/03/01
Cayman Chemical
Product number
28442
Product name
NBI 74330
Packaging
5mg
Price
$1253
Updated
2024/03/01
ChemScene
Product number
CS-2217
Product name
NBI-74330
Purity
99.23%
Packaging
100mg
Price
$1350
Updated
2021/12/16
ChemScene
Product number
CS-2217
Product name
NBI-74330
Purity
99.23%
Packaging
10mg
Price
$250
Updated
2021/12/16
ChemScene
Product number
CS-2217
Product name
NBI-74330
Purity
99.23%
Packaging
50mg
Price
$850
Updated
2021/12/16
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NBI-74330 Chemical Properties,Usage,Production

Description

NBI 74330 is a chemokine (C-X-C motif) receptor 3 (CXCR3) antagonist (Ki = 3.6 nM in a radioligand binding assay). It inhibits calcium mobilization induced by chemokine (C-X-C motif) ligand 10 (CXCL10) or CXCL11 in RBL cells expressing human CXCR3 (IC50 = 7 nM for both). NBI 74330 inhibits CXCL11-induced chemotaxis of CXCR3-expressing H9 cells and PHA and IL-2 differentiated T cells (IC50s = 3.9 and 6.6 nM, respectively). In vivo, NBI 74330 (100 mg/kg) reduces peritoneal lymphocyte migration in a mouse model of peritonitis. It reduces the size and number of aortic arch atherosclerotic lesions in Ldlr-/- mice. NBI 74330 reduces spinal cord microglial activation and levels of CXCL4, CXCL9, and CXCL10 and decreases thermal and mechanical hyperalgesia in a rat model of chronic constriction injury-induced neuropathic pain.

Uses

N-[(1R)-1-[3-(4-Ethoxyphenyl)-3,4-dihydro-4-oxopyrido[2,3-d]pyrimidin-2-yl]ethyl]-4-fluoro-N-(3-pyridinylmethyl)-3-(trifluoromethyl)benzeneacetamide is a CXCR3 antagonist.

in vivo

NBI-74330 (100 mg/kg) results in the formation of an N-oxide metabolite, also an antagonist of CXCR3, in mice[2].
Mice treated with 100 mg/kg NBI-74330 (in 1% Na Doc in 0.5% 400Cp Methylcellulose) result in serum concentrations of approximately 1 μM. This concentration is sufficient to fully block the CXCR3 receptor in vivo[3].

IC 50

[125I]CXCL10-CXCR3: 1.5 nM (Ki, in CXCR3-CHO cell membranes); [125I]CXCL11-CXCR3: 3.2 nM (Ki, in CXCR3-CHO cell membranes)

References

[1] CHRISTOPHER E HEISE. Pharmacological characterization of CXC chemokine receptor 3 ligands and a small molecule antagonist.[J]. Journal of Pharmacology and Experimental Therapeutics, 2005, 313 3: 1263-1271. DOI: 10.1124/jpet.105.083683
[2] EVA J A VAN WANROOIJ. CXCR3 antagonist NBI-74330 attenuates atherosclerotic plaque formation in LDL receptor-deficient mice.[J]. Arteriosclerosis, Thrombosis, and Vascular Biology, 2008: 251-257. DOI: 10.1161/atvbaha.107.147827
[3] ANNA PIOTROWSKA . Pharmacological blockade of CXCR3 by (±)-NBI-74330 reduces neuropathic pain and enhances opioid effectiveness - Evidence from in vivo and in vitro studies[J]. Biochimica et biophysica acta. Molecular basis of disease, 2018, 1864 10: Pages 3418-3437. DOI: 10.1016/j.bbadis.2018.07.032

NBI-74330 Preparation Products And Raw materials

Raw materials

Preparation Products

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NBI-74330 Suppliers

CHINA 40 United States 7 Global 47
Haoyuan Chemexpress Co., Ltd.
Tel
021-58950125
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(86) 21-58955996
Email
info@chemexpress.com
Country
China
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7552
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MedChemexpress LLC
Tel
021-58955995
Fax
609-228-5909
Email
sales@medchemexpress.cn
Country
United States
ProdList
4861
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58
Bide Pharmatech Ltd.
Tel
400-400-164-7117 18317119277
Fax
+86-21-61629029
Email
product02@bidepharm.com
Country
China
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39999
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SPIRO PHARMA
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Fax
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eric_feng1954@126.com
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China
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Shanghai EFE Biological Technology Co., Ltd.
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021-65675885 18964387627
Fax
021-65675885
Email
info@efebio.com
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China
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9803
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Guangzhou QiYun Biotechnology Co., Ltd.
Tel
020-61288194 61288195
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020-61288700
Email
505721671@qq.com
Country
China
ProdList
3866
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58
Shanghai YuanYe Biotechnology Co., Ltd.
Tel
021-61312847; 18021002903
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QQ:3008007432
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3008007409@qq.com
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China
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86249
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Amadis Chemical Company Limited
Tel
571-89925085
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0086-571-89925065
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sales@amadischem.com
Country
China
ProdList
131957
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58
Musechem
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+1-800-259-7612
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+1-800-259-7612
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info@musechem.com
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United States
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4660
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InvivoChem
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+1-708-310-1919 +1-13798911105
Fax
708-557-7486
Email
sales@invivochem.cn
Country
United States
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6391
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855527-92-3, NBI-74330Related Search:

Sulfanilamide (2R,3S/2S,3R)-2-(2,4-DIFLUOROPHENYL)-3-(5-FLUORO-4-PYRIMIDINYL)-1-(1H-1,2,4-TRIAZOL-1-YL)-2-BUTANOL N-ACETYLLACTOSAMINE 2-Ethoxyethanol

  • NBI-74330
  • N-[(1R)-1-[3-(4-Ethoxyphenyl)-3,4-dihydro-4-oxopyrido[2,3-d]pyrimidin-2-yl]ethyl]-4-fluoro-N-(3-pyridinylmethyl)-3-(trifluoromethyl)benzeneacetamide
  • Benzeneacetamide, N-[(1R)-1-[3-(4-ethoxyphenyl)-3,4-dihydro-4-oxopyrido[2,3-d]pyrimidin-2-yl]ethyl]-4-fluoro-N-(3-pyridinylmethyl)-3-(trifluoromethyl)-
  • (R)-N-(1-(3-(4-Ethoxyphenyl)-4-oxo-3,4-dihydropyrido[2,3-d]pyrimidin-2-yl)ethyl)-2-(4-fluoro-3-(trifluoromethyl)phenyl)-N-(pyridin-3-ylmethyl)acetamide
  • N-{1-[3-(4-ethoxyphenyl)-4-oxo-3,4-dihydropyrido[2,3-d]pyrimidin- 2-yl]ethyl}-2-[4-fluoro-3-(trifluoromethyl)phenyl]-n-(3-pyridinyl Methyl)acetamide
  • 855527-92-3
  • C32H27F4N5O3