CK-102
CK-102 is an interleukin-1 (IL-1) inhibitor. CK-102 reduces mRNA synthesis. CK-102 does not inhibit DNA synthesis. CK-102 only slightly inhibits protein synthesis, or has no effect on it. CK-102 delays wound healing after ophthalmic surgery and prolongs the failure time of trabeculectomy fistulas. CK-102 inhibits lens protein-induced ocular inflammation at both early and late stages. CK-102 inhibits endotoxin-induced uveitis. CK-102 does not inhibit interleukin-1-induced uveitis. CK-102 can be used in research related to glaucoma filtration failure and uveitis.
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- CAS No.: 6236-97-1
- 화학식: C15H13NO
- 분자량:223.28
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
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Biological Activity
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IL-1 |
CK-102 (10-100 μg/mL; 24-72 h) inhibits proliferation of SIRC rabbit corneal fibroblast cells in a non-cytolytic manner, with viable cell counts remaining at or above initial levels while growing more slowly than controls across 10, 30, and 100 μg/mL concentrations at 24, 48, and 72 h[1].
CK-102 (10-100 μg/mL; 24-72 h) produces limited, inconsistent inhibition of DNA synthesis, transient inhibition of RNA synthesis at 24 and 48 h, and variable effects on protein synthesis (with occasional reduction or increase) in SIRC rabbit corneal fibroblast cells across 10, 30, and 100 μg/mL concentrations at 24, 48, and 72 h[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SIRC rabbit corneal fibroblast cells
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Concentration:10 μg/mL; 30 μg/mL; 100 μg/mL
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Incubation Time:24 h; 48 h; 72 h
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Result:Reduced viable cell numbers compared to controls at each time point.
Inhibited cell proliferation, with growth reduced initially but recovering later and proceeding at a slower rate than controls.
Maintained viable cell counts at or above the starting cell count, confirming no cytolytic effect.
CK-102 (1%; topical; single instillation; 1 hour prior to lens protein challenge) significantly suppresses both early and late phases of lens protein-induced uveitis in Oryctolagus cuniculus, with comparable efficacy to Prednisolone (HY-17463)[3].
CK-102 (10 mg/kg; i.p.; three times daily) significantly suppresses endotoxin-induced uveitis in rats, with greater potency than Prednisolone at an equivalent dose[3].
CK-102 (10 mg/kg; i.p.; three times daily) does not suppress interleukin-1-induced uveitis in rats[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Dutch Belted (adult, specific pathogen free for Pasteurellosis, glaucoma model via bilateral partial thickness trabeculectomy filtration surgery)[2]
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Dosage:10 mg
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Administration:subTenons injection; single dose; immediately after surgery
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Result:Prolonged the mean number of days to filtration fistula failure by 30% compared to vehicle control, with statistical significance.
Showed no side effects at the tested dose.
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Animal Model:New Zealand albino rabbits (either sex, 2.0 to 3.0 kg)[3]
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Dosage:1%
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Administration:topical; single instillation; 1 hour prior to lens protein challenge
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Result:Significantly suppressed fluorescein concentration (a marker of inflammation) in the anterior chamber at all measured time points (30, 60, 120, 180, 240, 300, 360 minutes) compared to solvent control, with mean values consistently lower than control.
Suppressed both early (0-3 hour) and late (4-5 hour) phases of inflammation.
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Animal Model:Sprague-Dawley rats (250-350 grams)[3]
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Dosage:10 mg/kg
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Administration:i.p.; three times daily; at 0, 4, and 10 hours after endotoxin injection
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Result:Significantly suppressed uveitis responses (measured via fluorescein concentration) at 1.5, 2, 3, 4, 5, and 6 hours after fluorescein injection, with mean fluorescein concentrations consistently lower than control.
Observed no obvious side effects during the experiment.
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Animal Model:Sprague-Dawley rats (250-350 grams)[3]
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Dosage:10 mg/kg
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Administration:i.p.; three times daily; at 0, 4, and 10 hours after interleukin-1 injection
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Result:Did not significantly affect interleukin-1-induced uveitis; fluorescein concentrations in treated rats were not statistically different from control values at any measured time point.
Chemical Information
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CAS No. 6236-97-1
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분자량 223.28
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화학식 C15H13NO
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SMILES
O=C1C=2C=CC=CC2NC=3C1=CC=C(C3C)C
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[1]. Chen Z, et al. Inhibitory effects of interleukin-1 blockers on corneal fibroblast proliferation. J Ocul Pharmacol Ther. 1996;12(2):169-182. [Content Brief]
[2]. Schwade ND, et al. Effects of interleukin-1 blockers on ophthalmic wound healing in a rabbit model of trabeculectomy. J Ocul Pharmacol Ther. 1995;11(2):125-134. [Content Brief]
[3]. Chiou GC, et al. Prevention and treatment of ocular inflammation with a new class of non-steroidal anti-inflammatory agents. J Ocul Pharmacol. 1994;10(1):335-347. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CK-102 Related Classifications
HY-121303 Related Classifications
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- CK-102
- 6236-97-1
- CK102
- CK 102
- Interleukin Related
- DNA/RNA Synthesis
- endotoxin-induced uveitis
- interleukin-1
- fibroblast proliferation
- SIRC rabbit corneal fibroblast cells
- trabeculectomy fistula failure
- corneal fibroblasts
- Dutch Belted rabbits
- ocular inflammation
- uveitis
- glaucoma filtration failure
- Inhibitor
- inhibitor
- inhibit