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| 1mg |
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| 5mg |
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| 10mg | |||
| Other Sizes |
| Targets |
The primary target of TIP 39 is the parathyroid hormone 2 receptor (PTH2R), a G protein-coupled receptor that is predominantly expressed in the brain. TIP 39 acts as a potent and selective agonist of the PTH2 receptor, with no significant activity at the PTH1 receptor. Upon binding to PTH2R, TIP 39 activates intracellular signaling pathways, including the cAMP/PKA pathway, which mediates its physiological effects. The receptor is involved in the regulation of pain, stress responses, and neuroendocrine function. TIP 39's selectivity for PTH2R over PTH1R makes it a valuable tool for studying the specific functions of this receptor.
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| ln Vitro |
In vitro, TIP 39 is a potent and selective agonist of the parathyroid hormone 2 receptor (PTH2R). It binds to PTH2R with high affinity and activates downstream signaling pathways, such as the cAMP/PKA pathway. The peptide's activity is concentration-dependent, with effects observed at nanomolar concentrations. TIP 39 has no significant activity at the PTH1 receptor, demonstrating its selectivity for PTH2R. The peptide is used in receptor binding and functional assays to study the pharmacology of PTH2R and to identify other ligands that may interact with this receptor. It is also used to investigate the physiological roles of PTH2R in various cell types.
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| ln Vivo |
In vivo, TIP 39 is involved in the regulation of pain, stress responses, and neuroendocrine function. Studies have shown that TIP 39 modulates pain perception, with analgesic effects observed in animal models. It also plays a role in the regulation of the hypothalamic-pituitary-adrenal (HPA) axis, influencing stress responses. TIP 39's expression in the hypothalamus suggests that it may be involved in the regulation of feeding behavior and energy homeostasis. The peptide's in vivo effects are mediated through its action on PTH2R in the brain. Further studies are needed to fully characterize its physiological roles and therapeutic potential.
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| Enzyme Assay |
Cell-free receptor binding assays for TIP 39 typically involve incubating the peptide with membranes from cells expressing the parathyroid hormone 2 receptor (PTH2R) and a radiolabeled ligand (e.g., [125I]-TIP 39). Bound and free ligand are separated by filtration, and the radioactivity is measured by gamma counting. The binding affinity (Kd) and receptor density (Bmax) are determined by Scatchard analysis. For functional assays, the peptide's ability to activate PTH2R is assessed by measuring cAMP accumulation in membrane preparations using a radioimmunoassay or ELISA. The EC50 value is determined by plotting the cAMP production against the peptide concentration.
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| Cell Assay |
For in vitro cellular experiments, cells expressing the parathyroid hormone 2 receptor (e.g., transfected cell lines, primary neuronal cultures) are cultured in appropriate media and treated with TIP 39 at various concentrations (typically 0.1-1000 nM). The peptide's ability to activate the receptor is assessed by measuring downstream signaling, such as cAMP accumulation using ELISA or radioimmunoassay. The duration of treatment varies depending on the specific assay. The peptide can also be used in competition assays with other PTH2R ligands to determine its relative affinity and potency.
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| Animal Protocol |
In vivo animal experiments with TIP 39 typically involve intracerebroventricular (ICV) or intravenous administration in rodents. A common protocol involves injecting the peptide into the lateral ventricle of the brain or into the bloodstream, and measuring its effects on pain perception (e.g., using the hot plate or tail-flick test), stress responses (e.g., measuring corticosterone levels), or neuroendocrine function. The dosage and route of administration vary depending on the specific experimental objectives. Blood and brain tissue samples are collected for biochemical and histological analysis.
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| ADME/Pharmacokinetics |
TIP 39 is a 39-amino acid peptide with a molecular weight of approximately 4500 g/mol. As a peptide, its pharmacokinetic properties are characterized by rapid clearance from the circulation due to proteolytic degradation. The peptide is typically administered by injection in preclinical studies. Its half-life is short, and it is rapidly metabolized by peptidases in the blood and tissues. The peptide is stable in lyophilized form and should be stored at -20degC. It is soluble in aqueous buffers. Its pharmacokinetic properties make it suitable for acute pharmacological studies but less suitable for chronic dosing.
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| Toxicity/Toxicokinetics |
The toxicity profile of TIP 39 has not been extensively characterized. As a naturally occurring neuropeptide, it is expected to have low toxicity at pharmacological doses. However, high doses may cause alterations in pain perception, stress responses, or neuroendocrine function due to its interaction with PTH2R. The compound should be handled with standard laboratory precautions and is intended for research use only.
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| References | |
| Additional Infomation |
TIP 39, Tuberoinfundibular Neuropeptide (CAS 277302-47-3), is a 39-amino acid neuropeptide that acts as a potent and selective agonist of the parathyroid hormone 2 receptor (PTH2R). It is primarily expressed in the brain and is involved in the regulation of pain, stress responses, and neuroendocrine function. TIP 39 has no significant activity at the PTH1 receptor, demonstrating its selectivity for PTH2R. The peptide is a valuable research tool for studying the PTH2 receptor and its physiological roles. It is available as a research compound and is not approved for clinical use.
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| Molecular Weight |
0
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|---|---|
| Exact Mass |
4503.434
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| CAS # |
277302-47-3
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| PubChem CID |
131637132
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| Appearance |
White to off-white solid powder
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| LogP |
-8.6
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| Hydrogen Bond Donor Count |
67
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| Hydrogen Bond Acceptor Count |
64
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| Rotatable Bond Count |
153
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| Heavy Atom Count |
318
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| Complexity |
11000
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| Defined Atom Stereocenter Count |
39
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| SMILES |
C[C@@H](C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC2=CNC=N2)C(=O)N[C@@H](CC3=CNC4=CC=CC=C43)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC5=CC=C(C=C5)O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC6=CNC=N6)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N7CCC[C@H]7C(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)N
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| InChi Key |
TYWILDUTZVAJDB-IESKOEEDSA-N
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| InChi Code |
InChI=1S/C202H325N61O54S/c1-96(2)71-132(243-164(283)111(26)232-177(296)133(72-97(3)4)247-166(285)121(204)92-264)176(295)231-112(27)165(284)246-149(88-157(276)277)192(311)259-147(86-155(272)273)179(298)230-107(22)160(279)227-109(24)163(282)245-141(80-114-43-31-30-32-44-114)186(305)239-127(51-40-67-221-201(212)213)169(288)240-129(58-60-153(268)269)173(292)235-124(48-37-64-218-198(206)207)167(286)228-110(25)161(280)234-125(49-38-65-219-199(208)209)171(290)249-136(75-100(9)10)182(301)250-134(73-98(5)6)178(297)229-106(21)159(278)226-108(23)162(281)244-135(74-99(7)8)181(300)241-130(59-61-154(270)271)174(293)237-126(50-39-66-220-200(210)211)168(287)236-128(52-41-68-222-202(214)215)172(291)255-145(84-118-91-217-95-225-118)190(309)254-143(82-116-89-223-122-46-34-33-45-120(116)122)188(307)251-138(77-102(13)14)184(303)257-146(85-152(205)267)191(310)261-150(93-265)194(313)253-142(81-115-54-56-119(266)57-55-115)187(306)242-131(62-70-318-29)175(294)256-144(83-117-90-216-94-224-117)189(308)238-123(47-35-36-63-203)170(289)248-137(76-101(11)12)183(302)252-140(79-104(17)18)193(312)262-158(105(19)20)195(314)260-139(78-103(15)16)185(304)258-148(87-156(274)275)180(299)233-113(28)196(315)263-69-42-53-151(263)197(316)317/h30-34,43-46,54-57,89-91,94-113,121,123-151,158,223,264-266H,35-42,47-53,58-88,92-93,203-204H2,1-29H3,(H2,205,267)(H,216,224)(H,217,225)(H,226,278)(H,227,279)(H,228,286)(H,229,297)(H,230,298)(H,231,295)(H,232,296)(H,233,299)(H,234,280)(H,235,292)(H,236,287)(H,237,293)(H,238,308)(H,239,305)(H,240,288)(H,241,300)(H,242,306)(H,243,283)(H,244,281)(H,245,282)(H,246,284)(H,247,285)(H,248,289)(H,249,290)(H,250,301)(H,251,307)(H,252,302)(H,253,313)(H,254,309)(H,255,291)(H,256,294)(H,257,303)(H,258,304)(H,259,311)(H,260,314)(H,261,310)(H,262,312)(H,268,269)(H,270,271)(H,272,273)(H,274,275)(H,276,277)(H,316,317)(H4,206,207,218)(H4,208,209,219)(H4,210,211,220)(H4,212,213,221)(H4,214,215,222)/t106-,107-,108-,109-,110-,111-,112-,113-,121-,123-,124-,125-,126-,127-,128-,129-,130-,131-,132-,133-,134-,135-,136-,137-,138-,139-,140-,141-,142-,143-,144-,145-,146-,147-,148-,149-,150-,151-,158-/m0/s1
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| Chemical Name |
(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-hydroxypropanoyl]amino]-4-methylpentanoyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]propanoyl]amino]-3-carboxypropanoyl]amino]-3-carboxypropanoyl]amino]propanoyl]amino]propanoyl]amino]-3-phenylpropanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-carboxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]propanoyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]hexanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-3-carboxypropanoyl]amino]propanoyl]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, 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) |
H2O : ~50 mg/mL (~11.10 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.) |
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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