| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| Other Sizes |
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| Targets |
IC50: 8.6 nM (Gαi1) and 166 nM (β-arrestin-2)[1]
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|---|---|
| ln Vitro |
The radioligand apelin-13 [Glp65, Nle75 with Ki of 0.93 nM >, tyrosine 77][125I][1] is bound by Elabela (19-32) (analogue 3). When HA-hAPJ receptor is transiently expressed in HEK293 cells, Elabela (19-32) exhibits an EC50 of 36 nM. Apelin-13 and ELA are slightly more effective than Elabela (19-32) at starting receptor internalization [1]. With an EC50 of 1.5 pM, Elabela (19-32) (0.001 to 0.3 nM) alters left ventricular developed pressure (LVDP) in isolated rat hearts that are perfused with Langendorff [1].
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| ln Vivo |
Rat plasma quickly metabolizes Elabela (19-32) (analog 3) (t1/2<2 minutes) [1].
|
| References |
[1]. Alexandre Murza, et al. Discovery and Structure-Activity Relationship of a Bioactive Fragment of ELABELA That Modulates Vascular and Cardiac Functions. J Med Chem. 2016 Apr 14;59(7):2962-72.
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| Molecular Formula |
C75H119N25O17S2
|
|---|---|
| Molecular Weight |
1707.03
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| CAS # |
1886973-05-2
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| Related CAS # |
Elabela(19-32) TFA
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| SMILES |
S(C)CC[C@@H](C(N1CCC[C@H]1C(N[C@H](C(N[C@H](C(N[C@@H](CO)C(N[C@@H](CCC/N=C(\N)/N)C(N[C@@H](C(C)C)C(N1CCC[C@H]1C(N[C@@H](CC1C=CC=CC=1)C(N1CCC[C@H]1C(=O)O)=O)=O)=O)=O)=O)=O)CC1=CN=CN1)=O)CC(C)C)=O)=O)NC([C@H](CS)NC([C@H](CCC/N=C(\N)/N)NC([C@H](CCC/N=C(\N)/N)NC([C@@H]1CCC(N1)=O)=O)=O)=O)=O
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| 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) |
H2O: 100 mg/mL (58.58 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 50 mg/mL (29.29 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 | 0.5858 mL | 2.9291 mL | 5.8581 mL | |
| 5 mM | 0.1172 mL | 0.5858 mL | 1.1716 mL | |
| 10 mM | 0.0586 mL | 0.2929 mL | 0.5858 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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