| Identification | Back Directory | [Name]
CP-105,696 | [CAS]
158081-99-3 | [Synonyms]
CP-105,696
Pfizer 105696
UNII-Z7354TW4BM
CP-105,696 >=98% (HPLC)
CP 105696; CP105696; CP-105696; UNII-Z7354TW4BM; PFIZER 105696
1-((3S,4R)-3-([1,1'-biphenyl]-4-ylmethyl)-4-hydroxychroman-7-yl)cyclopentane-1-carboxylic acid
1-[(3S,4R)-4-hydroxy-3-[(4-phenylphenyl)methyl]-3,4-dihydro-2H-chromen-7-yl]cyclopentane-1-carboxylic acid
Cyclopentanecarboxylic acid, 1-[(3S,4R)-3-([1,1'-biphenyl]-4-ylmethyl)-3,4-dihydro-4-hydroxy-2H-1-benzopyran-7-yl]- | [Molecular Formula]
C28H28O4 | [MDL Number]
MFCD00934881 | [MOL File]
158081-99-3.mol | [Molecular Weight]
428.52 |
| Chemical Properties | Back Directory | [Boiling point ]
651.2±55.0 °C(Predicted) | [density ]
1.252±0.06 g/cm3(Predicted) | [storage temp. ]
room temp | [solubility ]
Soluble in DMSO | [form ]
powder | [pka]
4.35±0.20(Predicted) | [color ]
white to beige | [InChIKey]
KMNLXCBYBKHKSK-BKMJKUGQSA-N | [SMILES]
C1(C2=CC=C3C(=C2)OC[C@H](CC2=CC=C(C4=CC=CC=C4)C=C2)[C@H]3O)(C(O)=O)CCCC1 |
| Hazard Information | Back Directory | [Uses]
CP-105,696 has been used as a leukotriene B4 receptor (LTB4R) antagonist to study the influence of the LTB4 pathway in the pathogenesis of acute itch flares in irritant calcipotriol (MC903)+ model allergen ovalbumin (OVA) sensitized murine model of atopic dermatitis (AD)-like disease. | [Biochem/physiol Actions]
CP-105,696 is an orally active, potent and selective leukotriene B4 receptor (LTB4R) antagonist (IC50 against [3H]LTB4 = 5.6 nM for binding human neutrophils; IC50 = 9.7 nM & 30.3 nM, respectively using guinea pig spleen or mouse membranes) that targets LTB4R high- and low-affinity binding sites in a LTB4 non-competitive and competitive manner, respectively. CP-105,696 inhibits 5 nM LTB4-induced human neutrophils chemotaxis and CDllb upregualtion (IC50 = 5.2 nM and 430 nM, respectively) without inhibiting cyclooxygenase activity or affecting chemotaxis induced by C5a, PAF, IL-8. Oral administration is efficacious against intradermal LTB4 (100 ng/mouse), but not IL-1, injection-induced neutrophil accumulation in mice and guinea pigs (ED50 = 4.2 and 0.26 mgkg, respectively). CP-105,696 in vivo efficacy is also demonstrated in other animal models, including collagen-induced arthritis (CIA; 0.3-10 mg/kg in mice), allergic encephalomyelitis (ED50= 8.6 mg/kg; mice), and asthma (10-30 mg/kg; primate). | [in vivo]
At a dose of 50 mg/kg/day (28 days), B10.BR (H2k) allografts transplanted into C57Bl/6 (H2b) recipients are significantly protected, as reflected by the mean survival time versus control grafts (27±20 days [n=10] vs. 12±6 days [n=14]; P=0.0146). Using an induction protocol (day -1 to day 3), CP-105696 at 100 mg/kg/day significantly prolongs allograft survival (33±23 days [n=9]; P=0.0026), but CP-105696 at 10 mg/kg/day does not (18±16 days [n=8]; P=0.1433). Syngeneic grafts survive indefinitely (n=11). Immunohistological evaluation of allografts at rejection reveals a mononuclear cell infiltrate composed primarily of CD3+ and CD11b+ (Mac-1+) cells, which are infrequent in syngeneic grafts. Allografts from mice treated with CP-105696 at 50 or 100 mg/kg/day demonstrat a selective reduction in β2-integrin (Mac-1) expression on monocytes/macrophages, as demonstrated by CD11b staining density compared with allograft controls[2]. | [IC 50]
LTB4: 8.42±0.26 nM (IC50) |
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| Company Name: |
Sigma-Aldrich
|
| Tel: |
021-61415566 800-8193336 |
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https://www.sigmaaldrich.cn |
| Company Name: |
Twochem Co.Ltd.
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021-58111628 15800915896 |
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cn.twochem.com |
| Company Name: |
Energy Chemical
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021-58432009 400-005-6266 |
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http://www.energy-chemical.com |
| Company Name: |
cjbscvictory
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13348960310 13348960310; |
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https://www.weikeqi-biotech.com/ |
| Company Name: |
InvivoChem
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13549236410 |
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https://www.invivochem.cn/ |
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