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| 5mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
UK-371804 is a potent and selective inhibitor of urokinase-type plasmogen activator (uPA) with excellent potency (Ki=10 nM in an enzyme assay) and selectivity profile (4000-fold versus tPA and 2700-fold versus plasmin). In vitro, UK-371804 can inhibit exogenous uPA in human chronic wound fluid (IC50=0.89 microM). Following topical application, UK-371804 is able to penetrate into pig wounds in a porcine acute excisional wound model in vivo and inhibit exogenous uPA activity without having an adverse effect on wound healing parameters.
| Targets |
uPA (Ki = 10 nM)
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|---|---|
| ln Vitro |
UK-3718046 (IC50=0.89 µM) has the ability to inhibit exogenous uPA in human chronic wound fluid in vitro[1].
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| ln Vivo |
UK-3718046 can penetrate pig wounds in a porcine acute excisional wound model in vivo and inhibit exogenous uPA activity without negatively affecting wound healing parameters after topical administration[1].
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| Enzyme Assay |
UK-371804 has an IC50 of 0.89 μM for inhibiting exogenous uPA in human chronic wound fluid. UK-371804 has a remarkable selectivity profile (4000-fold versus tPA and 2700-fold versus plasmin) and excellent enzyme potency (Ki=10nM).
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| Animal Protocol |
A porcine acute excisional wound model
10 mg/mL topical delivery |
| References |
| Molecular Formula |
C14H16CLN5O4S.HCL
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|---|---|---|
| Molecular Weight |
422.29
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| Exact Mass |
421.037
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| CAS # |
256476-36-5
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| Related CAS # |
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| PubChem CID |
16657953
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| Appearance |
Typically exists as solid at room temperature
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
26
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| Complexity |
644
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
IUBFETAFRGVODB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H16ClN5O4S.ClH/c1-14(2,12(21)22)20-25(23,24)7-3-4-8-9(5-7)11(19-13(16)17)18-6-10(8)15;/h3-6,20H,1-2H3,(H,21,22)(H4,16,17,18,19);1H
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| Chemical Name |
2-[[4-chloro-1-(diaminomethylideneamino)isoquinolin-7-yl]sulfonylamino]-2-methylpropanoic acid;hydrochloride
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3680 mL | 11.8402 mL | 23.6804 mL | |
| 5 mM | 0.4736 mL | 2.3680 mL | 4.7361 mL | |
| 10 mM | 0.2368 mL | 1.1840 mL | 2.3680 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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