| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| ln Vitro |
Proliferating cell nuclear antigen (PCNA) protein, which is increased by Ang II, is not expressed when Ang-(1–7) is inhibited, while A-779 by itself has little effect on causing VSMC migration and proliferation. A-779 blocks the effects of Ang-(1-7) on the VSMC inflammatory response, which is linked to the elevation of MCP-1, VCAM-1, and IL-1β production. Ang-(1-7) pretreatment can greatly delay this inflammatory response. But A-779 by itself was unable to cause VSMCs to become inflamed. VSMCs treated with Ang-(1-7) for 5 minutes prior to Ang II-induced activation of Akt and ERK1/2 was considerably reduced. A-779 also had this effect, although it did not cause Akt and ERK1 phosphorylation on its own. /2's function in VSMC[3].
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| ln Vivo |
For six weeks, OVX rats receiving an infusion of Ang(1-7) and A-779 (400?ng/kg/min, sc) either alone or in combination did not stop uterine atrophy or inhibit weight gain. Serum levels of type I collagen telopeptide (CTX), tartrate-resistant acid phosphatase (TRAcP 5b), osteocalcin (OC), urine deoxypyridine phenylin (DPD), and bone-specific alkaline phosphatase (BALP) are all markedly elevated by A-779. Serum mineral concentrations in the OVX or sham groups were not significantly changed by the infusion of Ang(1–7) and/or A-779. In contrast to the OVX group, A-779 in OVX animals did not change the expression of AngII, Ang(1-7), AT1R, AT2R, ACE, ACE-2, Mas receptor, RANKL, or OPG protein. However, A-779 (400ng/kg/min) significantly reduced the protective effects of captopril on bone metabolism, mineralization, and microstructure. A-779 also Restored the effect of OVX on RANKL expression ACE-1/AngII/AT1R cascade and downregulated OPG expression and ACE-2/Ang1-7/Mas pathway [2].
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| References |
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| Molecular Formula |
C39H60N12O11
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|---|---|
| Molecular Weight |
872.96700
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| Exact Mass |
872.45
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| CAS # |
159432-28-7
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| PubChem CID |
10169886
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Index of Refraction |
1.651
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| LogP |
0.3
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| Hydrogen Bond Donor Count |
13
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| Hydrogen Bond Acceptor Count |
14
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| Rotatable Bond Count |
26
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| Heavy Atom Count |
62
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| Complexity |
1570
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| Defined Atom Stereocenter Count |
8
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| SMILES |
CC[C@H](C)[C@@H](C(=O)N[C@@H](CC1=CN=CN1)C(=O)N[C@H](C)C(=O)O)NC(=O)[C@H](CC2=CC=C(C=C2)O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(=O)O)N
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| InChi Key |
GZSZZUXDAPDPOR-NGIFJXEWSA-N
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| InChi Code |
InChI=1S/C39H60N12O11/c1-6-20(4)31(37(60)49-28(15-23-17-43-18-45-23)34(57)46-21(5)38(61)62)51-35(58)27(14-22-9-11-24(52)12-10-22)48-36(59)30(19(2)3)50-33(56)26(8-7-13-44-39(41)42)47-32(55)25(40)16-29(53)54/h9-12,17-21,25-28,30-31,52H,6-8,13-16,40H2,1-5H3,(H,43,45)(H,46,57)(H,47,55)(H,48,59)(H,49,60)(H,50,56)(H,51,58)(H,53,54)(H,61,62)(H4,41,42,44)/t20-,21+,25-,26-,27-,28-,30-,31-/m0/s1
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| Chemical Name |
(3S)-3-amino-4-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(1R)-1-carboxyethyl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-oxobutanoic acid
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
0.1 M HCL : 25 mg/mL (~28.64 mM)
H2O : ~5 mg/mL (~5.73 mM) |
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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 | 1.1455 mL | 5.7276 mL | 11.4551 mL | |
| 5 mM | 0.2291 mL | 1.1455 mL | 2.2910 mL | |
| 10 mM | 0.1146 mL | 0.5728 mL | 1.1455 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05786729 | Enrolling by invitation | Other: Aerobic Exercise (AER) Other: Rehabilitation |
Traumatic Brain Injury | Centre for Neuro Skills | January 18, 2022 | Phase 1 Phase 2 |
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