| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| Targets |
PEN (human) specifically targets GPR83, an orphan G protein-coupled receptor that is predominantly expressed in the brain, particularly in the hypothalamus. This interaction has been identified as a key ligand-receptor pair in the central nervous system. By acting as an endogenous agonist, PEN plays a role in modulating neuroendocrine functions and potentially other central nervous system processes.
|
|---|---|
| ln Vitro |
Human PEN (hPEN) is more divergent and has the sequence PEG instead of PEN, while mouse PEN (mPEN) and rat PEN (rPEN) only differ by one residue at the N-terminal end[2]. In the brain, PEN attaches to and activates a GPCR[2].
In vitro, PEN (human) is a potent agonist at GPR83. Its activity has been characterized in cell-based assays, confirming its role as the endogenous ligand for this receptor. It is used to study GPR83-mediated signaling pathways and to investigate the physiological functions of this receptor system. The compound's high potency and specificity make it a key tool for probing GPR83 biology. |
| ln Vivo |
In vivo activity data for PEN (human) are not extensively detailed in the search results. As an endogenous neuropeptide, it is believed to play a role in the regulation of food intake and other neuroendocrine functions. It is used as a research tool to study the physiological and pathophysiological roles of the GPR83 receptor system in the brain.
|
| Enzyme Assay |
For non-cellular in vitro receptor binding assays, PEN (human) is used to characterize its binding affinity and selectivity for GPR83. Typically, this involves radioligand binding displacement assays using membrane preparations from cells expressing the receptor. Its identification as the endogenous ligand for GPR83 was confirmed through such studies.
|
| Cell Assay |
For in vitro cellular assays, the activity of PEN (human) is evaluated in cells expressing GPR83. A typical assay involves measuring the activation of downstream signaling pathways, such as the mobilization of intracellular calcium or the inhibition of cAMP accumulation, depending on the receptor's coupling. These assays confirm its agonistic activity and are used to study receptor pharmacology.
|
| Animal Protocol |
In vivo animal studies with PEN (human) are typically conducted in mouse models to investigate the role of GPR83 in various neuroendocrine functions. For example, it could be used to study its effects on food intake, energy homeostasis, or stress responses. The peptide can be administered via intracerebroventricular (ICV) injection to target the central nervous system directly.
|
| ADME/Pharmacokinetics |
Pharmacokinetic data for PEN (human) are not applicable as it is a research tool, not a therapeutic agent. As a neuropeptide, its half-life in the circulation is expected to be short due to rapid degradation by peptidases. For research purposes, it is typically administered directly into the brain (e.g., ICV) to bypass systemic clearance and ensure it reaches its target receptors in the central nervous system.
|
| Toxicity/Toxicokinetics |
Toxicological data for PEN (human) are not applicable. As a research compound, it is intended for laboratory use only and not for human therapeutic applications. Its safety profile has not been established for clinical use. At the concentrations used in research, it is generally considered to have low toxicity, but standard laboratory safety practices should always be followed.
|
| References | |
| Additional Infomation |
PEN (human) is an endogenous neuropeptide and a potent, selective agonist for the orphan G protein-coupled receptor GPR83. It is derived from the proSAAS proprotein and is one of the most abundant hypothalamic neuropeptides. It is a key research tool for studying GPR83 function in neuroendocrine signaling and the central nervous system. It has a molecular weight of 2215.49.
|
| Molecular Formula |
C97H159N27O32
|
|---|---|
| Molecular Weight |
2215.46208310127
|
| Exact Mass |
2215.167
|
| CAS # |
597578-70-6
|
| PubChem CID |
131648252
|
| Appearance |
White to off-white solid powder
|
| LogP |
-5.6
|
| Hydrogen Bond Donor Count |
30
|
| Hydrogen Bond Acceptor Count |
35
|
| Rotatable Bond Count |
70
|
| Heavy Atom Count |
156
|
| Complexity |
4970
|
| Defined Atom Stereocenter Count |
19
|
| SMILES |
C(N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)NCC(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@H](C(=O)O)C(C)C)([C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)CNC(=O)[C@H](C(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](N)C)CC1NC=NC=1)=O
|
| InChi Key |
PEIJMGIGWZOADR-UCVVRVGMSA-N
|
| InChi Code |
InChI=1S/C97H159N27O32/c1-44(2)31-58(82(141)104-39-68(126)107-52(16)79(138)113-59(32-45(3)4)86(145)115-60(33-46(5)6)85(144)110-55(21-18-28-102-97(99)100)84(143)122-77(50(13)14)96(155)156)118-93(152)76(49(11)12)120-70(128)41-103-81(140)56(24-26-71(129)130)112-91(150)66-22-19-29-123(66)95(154)67-23-20-30-124(67)94(153)64(34-47(7)8)119-83(142)57(25-27-72(131)132)111-90(149)65(42-125)109-69(127)40-105-92(151)75(48(9)10)121-89(148)63(37-74(135)136)117-87(146)61(35-54-38-101-43-106-54)116-88(147)62(36-73(133)134)114-80(139)53(17)108-78(137)51(15)98/h38,43-53,55-67,75-77,125H,18-37,39-42,98H2,1-17H3,(H,101,106)(H,103,140)(H,104,141)(H,105,151)(H,107,126)(H,108,137)(H,109,127)(H,110,144)(H,111,149)(H,112,150)(H,113,138)(H,114,139)(H,115,145)(H,116,147)(H,117,146)(H,118,152)(H,119,142)(H,120,128)(H,121,148)(H,122,143)(H,129,130)(H,131,132)(H,133,134)(H,135,136)(H,155,156)(H4,99,100,102)/t51-,52-,53-,55-,56-,57-,58-,59-,60-,61-,62-,63-,64-,65-,66-,67-,75-,76-,77-/m0/s1
|
| Chemical Name |
(4S)-4-[[(2S)-1-[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-aminopropanoyl]amino]propanoyl]amino]-3-carboxypropanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-3-carboxypropanoyl]amino]-3-methylbutanoyl]amino]acetyl]amino]-3-hydroxypropanoyl]amino]-4-carboxybutanoyl]amino]-4-methylpentanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]-5-[[2-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[(1S)-1-carboxy-2-methylpropyl]amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-2-oxoethyl]amino]-5-oxopentanoic acid
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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
|
|---|---|
| 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 | 0.4514 mL | 2.2569 mL | 4.5137 mL | |
| 5 mM | 0.0903 mL | 0.4514 mL | 0.9027 mL | |
| 10 mM | 0.0451 mL | 0.2257 mL | 0.4514 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
