| Size | Price | |
|---|---|---|
| 100mg | ||
| 250mg | ||
| 500mg | ||
| Other Sizes |
| Targets |
MMP-2 0.81 nM (IC50) MMP-13 0.56 nM (IC50) MMP-8 10.8 nM (IC50) MMP-9 18 nM (IC50) MMP-3 120 nM (IC50) MMP-1 1900 nM (IC50)
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|---|---|
| ln Vitro |
XL-784 is an extremely powerful MMP inhibitor with a low molecular weight of 1,122 g/mol and a very low solubility in water (20 μg/mL). With IC50 values between 1-2 nM, XL-784 potently inhibits the activity of MMP-2, MMP-13, and ADAM10 [TNF-α-converting enzyme (TACE)] in vitro. Additionally, MMP-9 (IC50 ~20 nM) and ADAM17 (IC50 ~70 nM), also referred to as TACE, are inhibited by XL-784. On the other hand, its MMP-1 inhibition potency is low (IC50 ~2,000 nM)[1].
|
| ln Vivo |
Every mouse reacts to the treatments in the same way. The aneurysms in all control mice had a mean percentageΔAD of 158.5%±4.3%. Inhibiting aortic dilatation is effective when XL-784 and doxycycline are used at all doses. A distinct dose-response association exists between and. The larger doses (375 mg/kg 88.6%±4.4% and 500 mg/kg 76.0%±3.5%) exhibit the same behavior. The two maximum XL-784 doses that were evaluated were shown to be more effective than doxycycline (112.2%±2.0%, P<0.05) in preventing the aorta from expanding to its maximum size following elastase perfusion[2].
|
| References |
[1]. Williams JM, et al. Evaluation of metalloprotease inhibitors on hypertension and diabetic nephropathy. Am J Physiol Renal Physiol. 2011 Apr;300(4):F983-98.
[2]. Ennis T, et al. Effect of novel limited-spectrum MMP inhibitor XL784 in abdominal aortic aneurysms. J Cardiovasc Pharmacol Ther. 2012 Dec;17(4):417-26 |
| Molecular Formula |
C21H22CLF2N3O8S
|
|---|---|
| Molecular Weight |
549.93
|
| CAS # |
1356992-21-6
|
| Related CAS # |
XL-784;1224964-36-6
|
| SMILES |
C1(=C(F)C=C(C=C1F)S(=O)(N1C(C(NO)=O)CN(CC1)C(OCCOC)=O)=O)OC1C=CC(Cl)=CC=1
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: 250 mg/mL (454.60 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.78 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.78 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (3.78 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8184 mL | 9.0921 mL | 18.1841 mL | |
| 5 mM | 0.3637 mL | 1.8184 mL | 3.6368 mL | |
| 10 mM | 0.1818 mL | 0.9092 mL | 1.8184 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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