| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vivo |
Apelin-13 (200 µg/kg; IP, once daily for 4 weeks) increases the levels of GLUT4 and p-AMPKα2, decreases serum TNF-α and leptin, enhances lipid metabolism, and improves cardiac function [2]. It also dramatically increases serum Apelin-12 expression. Most globus pallidus neurons exhibit increased spontaneous firing in response to Apelin-13 (10 and 100 μM; ICV, single dose) [4].
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|---|---|
| Animal Protocol |
Animal/Disease Models: Goto-Kakizaki (GK) rat (12 weeks old; 240-280 g; fed high-fat diet: 66.5% standard chow, 10% lard, 20% sucrose, 2.5% cholesterol, and 1% porcine bile salts) )[2]
Doses: 200 µg/kg Route of Administration: intraperitoneal (ip) injection, one time/day for 4 weeks Experimental Results: Significant reduction in heart rate; reduction in fasting plasma glucose (FPG), fasting insulin (FINS) and insulin resistance Homeostasis Model Assessment (HOMA-IR) levels; reduce serum total cholesterol (TC), triglyceride (TG) and low-density lipoprotein cholesterol (LDL-C) levels, and increase high-density lipoprotein cholesterol (HDL-C); in serum NO levels, cNOS activity, TNF-α and leptin were diminished; Apelin-12 expression was induced. Animal/Disease Models: Adult Wistar rat (SPF, 8-10 weeks, 240-280 g) [4] Doses: 10 and 100 μM Route of Administration: ICV, single dose Experimental Results: Increased spontaneous firing of most globus pallidus neurons. |
| References |
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| Additional Infomation |
Apelin-13 is a 13 amino acid oligopeptide which is the ligand for the apelin receptor (also known as the APJ receptor). It exhibits hypotensive and neuroprotective effects, and may be a potential prognostic biomarker for acute ischemic stroke and multiple sclerosis. It has a role as an antihypertensive agent, a biomarker, an autophagy inhibitor, a neuroprotective agent and a human metabolite. It is a conjugate base of an apelin-13(3+).
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| Molecular Formula |
C69H111N23O16S
|
|---|---|
| Molecular Weight |
1550.82914
|
| Exact Mass |
1549.829
|
| CAS # |
217082-58-1
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| Related CAS # |
Apelin-13 TFA
|
| PubChem CID |
25078060
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.5±0.1 g/cm3
|
| Index of Refraction |
1.688
|
| LogP |
-3.42
|
| Hydrogen Bond Donor Count |
19
|
| Hydrogen Bond Acceptor Count |
22
|
| Rotatable Bond Count |
47
|
| Heavy Atom Count |
109
|
| Complexity |
3140
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| Defined Atom Stereocenter Count |
12
|
| SMILES |
CC(C[C@H](NC([C@@H](NC([C@@H]1CCCN1C([C@@H](NC([C@@H](N)CCC(N)=O)=O)CCCNC(N)=N)=O)=O)CCCNC(N)=N)=O)C(N[C@H](C(N[C@H](C(N[C@H](C(NCC(N2CCC[C@H]2C(N[C@H](C(N3CCC[C@H]3C(N[C@H](C(O)=O)CC4=CC=CC=C4)=O)=O)CCSC)=O)=O)=O)CCCCN)=O)CC5=CN=CN5)=O)CO)=O)C
|
| InChi Key |
XXCCRHIAIBQDPX-PEWBXTNBSA-N
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| InChi Code |
InChI=1S/C69H111N23O16S/c1-39(2)32-47(86-58(98)44(17-9-26-78-68(73)74)83-63(103)52-20-12-29-91(52)65(105)45(18-10-27-79-69(75)76)84-56(96)42(71)22-23-54(72)94)59(99)89-50(37-93)61(101)87-48(34-41-35-77-38-81-41)60(100)82-43(16-7-8-25-70)57(97)80-36-55(95)90-28-11-19-51(90)62(102)85-46(24-31-109-3)66(106)92-30-13-21-53(92)64(104)88-49(67(107)108)33-40-14-5-4-6-15-40/h4-6,14-15,35,38-39,42-53,93H,7-13,16-34,36-37,70-71H2,1-3H3,(H2,72,94)(H,77,81)(H,80,97)(H,82,100)(H,83,103)(H,84,96)(H,85,102)(H,86,98)(H,87,101)(H,88,104)(H,89,99)(H,107,108)(H4,73,74,78)(H4,75,76,79)/t42-,43-,44-,45-,46-,47-,48-,49-,50-,51-,52-,53-/m0/s1
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| Chemical Name |
(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-1-[2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-(diaminomethylideneamino)-2-[[(2S)-1-[(2S)-5-(diaminomethylideneamino)-2-[[(2S)-2,5-diamino-5-oxopentanoyl]amino]pentanoyl]pyrrolidine-2-carbonyl]amino]pentanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxypropanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]hexanoyl]amino]acetyl]pyrrolidine-2-carbonyl]amino]-4-methylsulfanylbutanoyl]pyrrolidine-2-carbonyl]amino]-3-phenylpropanoic 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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 0.6448 mL | 3.2241 mL | 6.4482 mL | |
| 5 mM | 0.1290 mL | 0.6448 mL | 1.2896 mL | |
| 10 mM | 0.0645 mL | 0.3224 mL | 0.6448 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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