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| Targets |
Adropin (34-76) is the endogenous ligand for the orphan G protein-coupled receptor GPR19. GPR19 is predominantly expressed in the brain, particularly in the medial basal hypothalamus, and its activation mediates the central effects of adropin, including the inhibition of water drinking behavior. The biological effects of adropin are mediated through the activation of GPR19, which signals via the MAPK/ERK1/2 pathway. In addition to GPR19, adropin also modulates other signaling pathways, including the cAMP signaling pathway and the GLI1 signaling pathway. The peptide's effects on glucose metabolism are mediated through the inhibition of cAMP levels and suppression of glucose production in hepatocytes. Its anti-fibrotic effects are mediated through the inhibition of GLI1 signaling, a pathway involved in the activation of profibrotic genes. Adropin also enhances insulin-induced Akt phosphorylation and GLUT4 cell-surface expression, thereby improving insulin sensitivity. The peptide's regulation of fuel selection preferences in skeletal muscle is thought to be mediated through the activation of GPR19 and downstream signaling pathways.
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| ln Vitro |
In vitro, adropin (34-76) exhibits potent biological activities in various cell types. In primary cultured mouse hepatocytes, adropin (34-76) at a concentration of 100 nM for 3 hours inhibits glucose production. This hypoglycemic effect is attributed to the suppression of cAMP levels in hepatocytes. In human umbilical vein endothelial cells (HUVECs), treatment with adropin (34-76) at 10 ng/mL for 18 hours modulates endothelial function. The peptide exerts anti-fibrotic effects by inhibiting GLI1 signaling, as confirmed by ChIP-seq analysis showing adropin-induced changes in TGFβ/GLI1 signaling. Adropin (34-76) also increases insulin-induced Akt phosphorylation and cell-surface expression of GLUT4 in cells from diet-induced obesity (DIO) mice. In skeletal muscle cells, adropin regulates fuel selection preferences, promoting carbohydrate utilization over fat oxidation.
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| ln Vivo |
In vivo, adropin (34-76) has demonstrated significant therapeutic effects in animal models. In diet-induced obese (DIO) mice with insulin resistance, adropin treatment improves glucose tolerance, enhances insulin action, and augments metabolic flexibility towards glucose utilization. Adropin treatment in DIO mice ameliorates insulin resistance without affecting body weight. The peptide also reduces hepatosteatosis and insulin resistance in DIO mice. In a mouse model of permanent middle cerebral artery occlusion (pMCAO), intravenous administration of adropin (34-76) at a dose of 900 nmol/kg at the onset of ischemia significantly decreased brain infarct volume compared to vehicle-treated controls. Adropin treatment also resulted in molecular changes in the cerebral cortex, as analyzed 24 hours after pMCAO. In the context of water drinking behavior, adropin acts in the brain to inhibit water drinking, and this effect is mediated through GPR19 in the medial basal hypothalamus.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for adropin (34-76) typically involve radioligand binding studies using membrane preparations from cells expressing GPR19. The peptide's ability to displace a specific radiolabeled ligand from GPR19 is measured to determine its binding affinity. Functional assays, such as measuring cAMP accumulation, MAPK/ERK1/2 phosphorylation, or calcium mobilization, are used to confirm GPR19 activation. These assays help to characterize the interaction between adropin and its receptor GPR19 and to evaluate the potency and efficacy of the peptide as a GPR19 agonist.
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| Cell Assay |
In vitro cell-based assays for adropin (34-76) are conducted in various cell types, including primary hepatocytes, HUVECs, and skeletal muscle cells. For glucose production assays, primary mouse hepatocytes are treated with adropin (34-76) at 100 nM for 3 hours, and glucose production is measured. For endothelial function studies, HUVECs are treated with adropin at 10 ng/mL for 18 hours. For anti-fibrotic studies, cells are treated with adropin, and GLI1 signaling is assessed by ChIP-seq or other molecular analyses. For insulin sensitivity assays, cells are treated with adropin, and Akt phosphorylation and GLUT4 cell-surface expression are measured.
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| Animal Protocol |
In vivo animal studies for adropin (34-76) are conducted in rodent models. In diet-induced obesity (DIO) mice, adropin is typically administered via intraperitoneal or intravenous injection, and its effects on glucose tolerance, insulin sensitivity, and hepatosteatosis are assessed. In the pMCAO stroke model, adropin (900 nmol/kg) is administered intravenously at the onset of ischemia, and brain infarct volume and molecular changes are evaluated. For studies on water drinking behavior, adropin is administered centrally or peripherally, and water intake is measured.
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| ADME/Pharmacokinetics |
No detailed pharmacokinetic data are publicly available for adropin (34-76). As a peptide, its pharmacokinetic properties would be characterized by limited oral bioavailability and rapid clearance. Its ADME properties would be studied in preclinical models to guide in vivo experiments. For peptide therapeutics, factors such as half-life, volume of distribution, and proteolytic stability are key considerations.
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| Toxicity/Toxicokinetics |
No specific toxicity data are publicly available for adropin (34-76). As a peptide hormone, its toxicity profile is expected to be related to its mechanism of action. Standard safety assessments would be required for any therapeutic development.
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| Additional Infomation |
Adropin (34-76) is a synthetic peptide corresponding to the bioactive C-terminal fragment of the adropin protein. It is the endogenous ligand for the orphan GPCR GPR19 and plays critical roles in energy metabolism, insulin sensitivity, and endothelial function. The peptide has shown therapeutic potential in preclinical models of metabolic disorders and stroke. Adropin (34-76) is not approved for human therapeutic use and is strictly for research purposes. The amino acid sequence of adropin is identical across humans, mice, and rats.
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| Molecular Formula |
C190H293N55O68S2
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|---|---|
| Molecular Weight |
4499.82
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| Exact Mass |
4499.067
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| CAS # |
1802086-30-1
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| PubChem CID |
171042614
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
61
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| Rotatable Bond Count |
92
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| Heavy Atom Count |
315
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| Complexity |
11400
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| Defined Atom Stereocenter Count |
41
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| SMILES |
C[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N3CCC[C@H]3C(=O)NCC(=O)N4CCC[C@H]4C(=O)N[C@@H](CSSC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CO)CCCNC(=N)N)CO)CC5=CNC=N5)N)C(=O)N6CCC[C@H]6C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N7CCC[C@H]7C(=O)N8CCC[C@H]8C(=O)N9CCC[C@H]9C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CC1=CNC=N1)C(=O)N[C@@H](CCC(=O)O)C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CC1=CC=C(C=C1)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)N)C(=O)N1CCC[C@H]1C(=O)O)CO)CO)CC(=O)N)CO)CO)CCC(=O)O)CO)CC(C)C)CO)CC(=O)O)C(C)C)CC(=O)O
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| InChi Key |
HSJJHNVPBLCAEH-PLGVNXRWSA-N
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| InChi Code |
InChI=1S/C190H293N55O68S2/c1-90(2)63-109(157(280)216-108(42-47-139(195)258)183(306)245-62-24-36-137(245)189(312)313)219-158(281)110(64-91(3)4)220-160(283)112(66-96-37-39-99(256)40-38-96)222-167(290)118(76-246)208-141(260)74-202-151(274)103(43-48-143(262)263)211-161(284)114(68-98-73-200-89-205-98)223-171(294)125(83-253)232-179(302)133-32-18-56-239(133)182(305)107(26-12-14-52-192)215-155(278)104(41-46-138(194)257)213-177(300)134-33-21-59-242(134)187(310)136-35-23-61-244(136)188(311)135-34-22-60-243(135)181(304)95(10)207-152(275)101(25-11-13-51-191)209-154(277)106(45-50-145(266)267)214-176(299)131-30-20-58-241(131)186(309)128-87-315-314-86-100(193)150(273)218-113(67-97-72-199-88-204-97)162(285)229-120(78-248)168(291)210-102(27-15-53-201-190(197)198)153(276)226-119(77-247)166(289)206-94(9)149(272)217-117(71-147(270)271)165(288)236-148(93(7)8)180(303)225-116(70-146(268)269)164(287)231-122(80-250)170(293)221-111(65-92(5)6)159(282)228-121(79-249)169(292)212-105(44-49-144(264)265)156(279)227-123(81-251)172(295)234-127(85-255)185(308)240-57-19-31-132(240)178(301)224-115(69-140(196)259)163(286)230-124(82-252)173(296)233-126(84-254)184(307)238-55-17-28-129(238)174(297)203-75-142(261)237-54-16-29-130(237)175(298)235-128/h37-40,72-73,88-95,100-137,148,246-256H,11-36,41-71,74-87,191-193H2,1-10H3,(H2,194,257)(H2,195,258)(H2,196,259)(H,199,204)(H,200,205)(H,202,274)(H,203,297)(H,206,289)(H,207,275)(H,208,260)(H,209,277)(H,210,291)(H,211,284)(H,212,292)(H,213,300)(H,214,299)(H,215,278)(H,216,280)(H,217,272)(H,218,273)(H,219,281)(H,220,283)(H,221,293)(H,222,290)(H,223,294)(H,224,301)(H,225,303)(H,226,276)(H,227,279)(H,228,282)(H,229,285)(H,230,286)(H,231,287)(H,232,302)(H,233,296)(H,234,295)(H,235,298)(H,236,288)(H,262,263)(H,264,265)(H,266,267)(H,268,269)(H,270,271)(H,312,313)(H4,197,198,201)/t94-,95-,100-,101-,102-,103-,104-,105-,106-,107-,108-,109-,110-,111-,112-,113-,114-,115-,116-,117-,118-,119-,120-,121-,122-,123-,124-,125-,126-,127-,128-,129-,130-,131-,132-,133-,134-,135-,136-,137-,148-/m0/s1
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| Chemical Name |
(2S)-1-[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-6-amino-2-[[(2S)-5-amino-2-[[(2S)-1-[(2S)-1-[(2S)-1-[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-1-[(6S,12S,15S,18S,21S,27S,30S,33S,36S,39S,42S,45S,48S,51S,54S,57S,60S,63S,66S,69R,74R,77S)-69-amino-18-(2-amino-2-oxoethyl)-60-(3-carbamimidamidopropyl)-33-(2-carboxyethyl)-45,51-bis(carboxymethyl)-12,15,27,30,36,42,57,63-octakis(hydroxymethyl)-66-(1H-imidazol-4-ylmethyl)-54-methyl-39-(2-methylpropyl)-2,5,11,14,17,20,26,29,32,35,38,41,44,47,50,53,56,59,62,65,68,76-docosaoxo-48-propan-2-yl-71,72-dithia-1,4,10,13,16,19,25,28,31,34,37,40,43,46,49,52,55,58,61,64,67,75-docosazatetracyclo[75.3.0.06,10.021,25]octacontane-74-carbonyl]pyrrolidine-2-carbonyl]amino]-4-carboxybutanoyl]amino]hexanoyl]amino]propanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-3-hydroxypropanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-5-oxopentanoyl]pyrrolidine-2-carboxylic 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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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) |
DMSO: 100 mg/mL (22.22 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 | 0.2222 mL | 1.1112 mL | 2.2223 mL | |
| 5 mM | 0.0444 mL | 0.2222 mL | 0.4445 mL | |
| 10 mM | 0.0222 mL | 0.1111 mL | 0.2222 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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