| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
Neurotensin receptors (NTS1 and NTS2). JMV 449 acetate is a potent neurotensin receptor agonist, primarily acting at NTS1 to mediate central effects such as analgesia and hypothermia.
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| ln Vitro |
JMV 449 acetate shows an IC50 of 0.15 nM for inhibition of 125I-neurotensin binding to neonatal mouse brain membranes, indicating high-affinity binding to neurotensin receptors. It also has an EC50 of 1.9 nM in contracting the guinea-pig ileum, a functional bioassay for neurotensin receptor activation. These data demonstrate its potent agonist activity.
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| ln Vivo |
JMV 449 exhibits analgesic effects at 120 pmol/mouse; icv[2].
JMV 449 acetate (120 pmol/mouse; i.c.v.) shows a significant analgesic effect in male Swiss albino mice. It has highly potent and long-lasting hypothermic and analgesic effects in mice, as described in the literature. These in vivo effects are mediated through activation of central neurotensin receptors following intracerebroventricular administration. |
| Enzyme Assay |
Cell-free neurotensin receptor binding assays are performed using neonatal mouse brain membranes. Membranes are prepared by homogenization of whole neonatal mouse brain in 50 mM Tris-HCl (pH 7.4) containing protease inhibitors. Membrane preparations are incubated with 0.1 nM 125I-neurotensin and increasing concentrations of JMV 449 acetate (0.001-1000 nM) in binding buffer for 30-60 min at 25degC. Bound radioactivity is separated by filtration through GF/B filters. IC50 is calculated by nonlinear regression. The IC50 of JMV 449 acetate is 0.15 nM.
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| Cell Assay |
The guinea-pig ileum functional assay is used as a bioassay for neurotensin receptor activity. Segments of guinea-pig ileum (2-3 cm) are mounted in organ baths containing oxygenated Krebs buffer at 37degC. After equilibration, increasing concentrations of JMV 449 acetate (0.1-100 nM) are added cumulatively, and contractile responses are recorded isometrically. EC50 values are determined from concentration-response curves. JMV 449 acetate contracts the guinea-pig ileum with an EC50 of 1.9 nM.
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| Animal Protocol |
Animal/Disease Models: Male Swiss albino mice[1]
Doses: 120 pmol/mouse Route of Administration: Icv Experimental Results: demonstrated dose-response relation-ships for the analgesic effect. In vivo analgesic studies are conducted in male Swiss albino mice. JMV 449 acetate is dissolved in sterile saline or artificial cerebrospinal fluid. For central administration, 120 pmol of JMV 449 acetate (dissolved in 5-10 uL) is injected intracerebroventricularly (i.c.v.) into the lateral ventricle. Analgesia is assessed by the hot plate test (55degC) or tail-flick test at various time points (15, 30, 60, 120 min) post-injection. Hypothermic effects are monitored by measuring rectal body temperature. Dose-response relationships are established for analgesic effects. |
| ADME/Pharmacokinetics |
No specific pharmacokinetic data are reported for JMV 449 acetate in the literature. As a pseudopeptide, it has improved metabolic stability compared to native neurotensin, as suggested by its long-lasting in vivo effects. The molecular weight is 807.03 (as acetate salt; parent peptide MW 746.98). Water solubility: 100 mg/mL (123.91 mM). JMV 449 acetate is soluble in water and DMSO. Storage: -20degC, sealed, away from moisture. For i.c.v. administration, it is formulated in saline.
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| Toxicity/Toxicokinetics |
No specific toxicity data are reported for JMV 449 acetate. In published studies, at the dose used for analgesia (120 pmol/mouse, i.c.v.), no overt signs of toxicity or adverse behavioral effects were observed. However, comprehensive toxicological assessments (acute toxicity, repeat-dose toxicity, genotoxicity) have not been performed. The compound has not progressed to clinical trials.
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| References |
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| Additional Infomation |
Other information: JMV 449 acetate (CAS# 141863-45-8) is a research-grade peptide, not FDA-approved. Its sequence is H-Arg-Lys-Pro-Tyr-Ile-Leu-OH acetate salt. It is a potent neurotensin receptor agonist with IC50 of 0.15 nM for receptor binding and EC50 of 1.9 nM for ileum contraction. It has highly potent and long-lasting hypothermic and analgesic effects in the mouse. Synonyms: JMV 449 acetate. For research use only.
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| Exact Mass |
806.527
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|---|---|
| CAS # |
141863-45-8
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| Related CAS # |
JMV 449;139026-66-7
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| PubChem CID |
155981977
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
10
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| Hydrogen Bond Acceptor Count |
13
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| Rotatable Bond Count |
25
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| Heavy Atom Count |
57
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| Complexity |
1170
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| Defined Atom Stereocenter Count |
7
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| SMILES |
CC[C@H](C)[C@@H](C(=O)N[C@@H](CC(C)C)C(=O)O)NC(=O)[C@H](CC1=CC=C(C=C1)O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCCN)NC[C@H](CCCCN)N.CC(=O)O
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| InChi Key |
JWAZBOKEQASLBT-ULBMXYNPSA-N
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| InChi Code |
InChI=1S/C38H66N8O7.C2H4O2/c1-5-25(4)33(36(50)44-31(38(52)53)21-24(2)3)45-34(48)30(22-26-14-16-28(47)17-15-26)43-35(49)32-13-10-20-46(32)37(51)29(12-7-9-19-40)42-23-27(41)11-6-8-18-39;1-2(3)4/h14-17,24-25,27,29-33,42,47H,5-13,18-23,39-41H2,1-4H3,(H,43,49)(H,44,50)(H,45,48)(H,52,53);1H3,(H,3,4)/t25-,27-,29-,30-,31-,32-,33-;/m0./s1
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| Chemical Name |
acetic acid;(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-6-amino-2-[[(2S)-2,6-diaminohexyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic 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: 100 mg/mL (123.91 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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