| Size | Price | Stock | Qty |
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| ln Vitro |
DX600 (1 μM) has a pIC50 of 8.0 and reduces rhACE2 activity by 47%[4]. 42% of ACE2 activity in human mononuclear cells (MCNs) is inhibited by DX600 (10 μM) [4]. When LPS and osthole are present, DX600 (100 nM, 4 hours) inhibits the growth of NR 8383 cells and raises TNF-a and IL-6 levels in the supernatant [5].
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| ln Vivo |
In diabetic rats treated with streptozotocin, DX600 (5 μg/kg/day, intraperitoneally, everyday for 4 weeks) TFA exacerbates the cardiovascular dysfunction caused by diabetes[2]. In a rat thrombosis model, DX600 (0.1 µmol/L/kg, intravenous administration) TFA enhanced thrombus weight by 30%[5].
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| Animal Protocol |
Animal/Disease Models: STZ-treated diabetes rats[2]
Doses: 5 μg/kg/day Route of Administration: ip, daily for 4 weeks Experimental Results: Increased cardiac and renal NOX activity. |
| References |
[1]. Liao K, et al. Development of an enzymatic assay for the detection of neutralizing antibodies against therapeutic angiotensin-converting enzyme 2 (ACE2).J Immunol Methods. 2013 Mar 29;389(1-2):52-60.
[2]. Yousif MH, et al. Characterization of Angiotensin-(1-7) effects on the cardiovascular system in an experimental model of type-1 diabetes. Pharmacol Res. 2012 Sep;66(3):269-75. [3]. Svilenov HL, et al. Extrinsic stabilization of antiviral ACE2-Fc fusion proteins targeting SARS-CoV-2. Commun Biol. 2023 Apr 8;6(1):386. [4]. Joshi S, et al. Angiotensin converting enzyme versus angiotensin converting enzyme-2 selectivity of MLN-4760 and DX600 in human and murine bone marrow-derived cells. Eur J Pharmacol. 2016 Mar 5;774:25-33. [5]. Fraga-Silva RA, et al. ACE2 activation promotes antithrombotic activity. Mol Med. 2010 May-Jun;16(5-6):210-5. |
| Molecular Formula |
C141H185N35O40S2
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|---|---|
| Molecular Weight |
3074.33
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| CAS # |
478188-26-0
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| Related CAS # |
DX600 TFA
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| SMILES |
C([C@H]1C(N[C@H](C(N[C@H](C(N[C@@H](CSSC[C@@H](C(N[C@H](C(N2CCC[C@@]2([H])C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N2CCC[C@@]2([H])C(N1)=O)=O)CC1C=CC(=CC=1)O)=O)CC1C=CC(=CC=1)O)=O)CCCNC(N)=N)=O)CC(C)C)=O)=O)CO)=O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)C)CC1C=CC(=CC=1)O)CC1NC=NC=1)C(=O)N[C@@H]([C@H](O)C)C(=O)N[C@@H](CC1C=CC(=CC=1)O)C(N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)NCC(=O)NCC(=O)NCC(=O)N)=O)=O)=O)CCCCN)=O)CC1=CNC2=CC=CC=C12)=O)C1=CNC2=CC=CC=C12
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| Solubility (In Vitro) |
H2O: 50 mg/mL (16.26 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 50 mg/mL (16.26 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.3253 mL | 1.6264 mL | 3.2527 mL | |
| 5 mM | 0.0651 mL | 0.3253 mL | 0.6505 mL | |
| 10 mM | 0.0325 mL | 0.1626 mL | 0.3253 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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