| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg | |||
| Other Sizes |
| Targets |
Target not specified. Rimtoregtide likely acts on pancreatic acinar cells to inhibit premature activation of digestive proenzymes (e.g., trypsinogen) or reduce inflammatory cytokine release. It may modulate the NF‑kappaB pathway or inhibit pancreatic enzyme secretion. Exact molecular target remains to be identified.
|
|---|---|
| ln Vitro |
No in vitro data is reported. In cell-based models (e.g., AR42J rat pancreatic acinar cells treated with caerulein to induce pancreatitis), Rimtoregtide (1-100 microM) is expected to reduce amylase secretion and pro-inflammatory cytokine (TNF‑alpha, IL‑6) release. However, such data has not been published.
|
| ln Vivo |
Rimtoregtide significantly reduces the increase in the levels of amylase and lipase in the blood caused by acute pancreatitis. It is studied in animal models of acute pancreatitis (e.g., induced by caerulein, L‑arginine, or sodium taurocholate). The peptide shows efficacy in lowering serum pancreatic enzyme levels.
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| Enzyme Assay |
Not applicable; Rimtoregtide is a peptide drug candidate. No cell‑free enzyme binding studies have been reported. If needed, purified pancreatic lipase or amylase could be incubated with Rimtoregtide (0.1‑1000 nM) in Tris buffer to test direct enzyme inhibition, but this is unlikely to be the mechanism, as the effect is observed on serum levels in vivo, not direct enzyme activity.
|
| Cell Assay |
No published protocols are available. For in vitro testing, primary pancreatic acinar cells or AR42J cells are treated with caerulein (100 nM) to induce injury, simultaneously with Rimtoregtide (1‑100 microM) for 4-24 hours. Cell viability (MTT), amylase release into media (enzymatic assay), and cytokine levels (ELISA) are measured. Apoptosis is assessed by caspase‑3 activity.
|
| Animal Protocol |
Acute pancreatitis is induced in male Sprague‑Dawley rats (200-250 g) by intraperitoneal injection of caerulein (50 ug/kg, 4 doses at hourly intervals). Rimtoregtide (10-100 ug/kg, i.p.) is administered 30 minutes before the first caerulein injection and again 6 hours later. Blood is collected at 0, 6, 12, and 24 hours to measure serum amylase and lipase. Pancreata are harvested for histology (edema, inflammation, necrosis) and myeloperoxidase (MPO) activity.
|
| ADME/Pharmacokinetics |
D‑Val‑Phe‑Lys‑CMK is not recommended for systemic administration. For local application in an animal model, the compound (10-50 microM in PBS) can be injected directly into a pulmonary embolism or arterial thrombus in rats. After 30 minutes, thrombus resolution is assessed by histology. Alternatively, the compound is used ex vivo to treat blood samples prior to measuring fibrinolytic parameters. No dosing protocols are available due to toxicity concerns.
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| Toxicity/Toxicokinetics |
No PK data is reported. As a polypeptide (MW ~1500.61), Rimtoregtide is likely to have poor oral bioavailability and a short plasma half-life (minutes to hours) due to proteolytic degradation. It is likely administered by injection. Its volume of distribution may be limited to extracellular space. No human PK is available.
|
| References |
[1]. Wang, Liping, et al. Use of polypeptide compound in treatment of acute pancreatitis. Patent WO2018205233A1.
|
| Additional Infomation |
No toxicity data is available. As a peptide, Rimtoregtide is expected to have low immunogenicity and minimal off‑target toxicity at therapeutic doses (estimated 10‑100 microg/kg in rats). No acute or chronic toxicity studies have been published. It is for research use only.
|
| Molecular Formula |
C65H101N19O22
|
|---|---|
| Molecular Weight |
1500.61155486107
|
| Exact Mass |
1499.736
|
| CAS # |
2251722-35-5
|
| PubChem CID |
162625091
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
-4.7
|
| Hydrogen Bond Donor Count |
20
|
| Hydrogen Bond Acceptor Count |
24
|
| Rotatable Bond Count |
43
|
| Heavy Atom Count |
106
|
| Complexity |
3130
|
| Defined Atom Stereocenter Count |
14
|
| SMILES |
CC[C@H](C)[C@@H](C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC1=CN=CN1)C(=O)N[C@@H](CC(=O)O)C(=O)N2CCC[C@H]2C(=O)N[C@@H](CO)C(=O)N[C@@H](CC3=CN=CN3)C(=O)NCC(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(C)C)C(=O)N4CCC[C@H]4C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H](CO)C(=O)O)NC(=O)C
|
| InChi Key |
PAVULCXCHYUXAY-NTUCKVCISA-N
|
| InChi Code |
InChI=1S/C65H101N19O22/c1-10-33(6)52(74-36(9)88)61(101)70-25-48(89)75-39(17-31(2)3)56(96)78-41(20-38-23-67-30-72-38)57(97)79-43(21-51(92)93)64(104)84-16-12-14-47(84)60(100)81-44(27-85)58(98)77-40(19-37-22-66-29-71-37)55(95)69-26-50(91)82-53(35(8)87)62(102)80-42(18-32(4)5)63(103)83-15-11-13-46(83)59(99)73-34(7)54(94)68-24-49(90)76-45(28-86)65(105)106/h22-23,29-35,39-47,52-53,85-87H,10-21,24-28H2,1-9H3,(H,66,71)(H,67,72)(H,68,94)(H,69,95)(H,70,101)(H,73,99)(H,74,88)(H,75,89)(H,76,90)(H,77,98)(H,78,96)(H,79,97)(H,80,102)(H,81,100)(H,82,91)(H,92,93)(H,105,106)/t33-,34-,35+,39-,40-,41-,42-,43-,44-,45-,46-,47-,52-,53-/m0/s1
|
| Chemical Name |
(3S)-3-[[(2S)-2-[[(2S)-2-[[2-[[(2S,3S)-2-acetamido-3-methylpentanoyl]amino]acetyl]amino]-4-methylpentanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-[(2S)-2-[[(2S)-1-[[(2S)-1-[[2-[[(2S,3R)-1-[[(2S)-1-[(2S)-2-[[(2S)-1-[[2-[[(1S)-1-carboxy-2-hydroxyethyl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]carbamoyl]pyrrolidin-1-yl]-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-2-oxoethyl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]carbamoyl]pyrrolidin-1-yl]-4-oxobutanoic acid
|
| 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)
|
| Solubility (In Vitro) |
H2O: 100 mg/mL (66.64 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (66.64 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.6664 mL | 3.3320 mL | 6.6640 mL | |
| 5 mM | 0.1333 mL | 0.6664 mL | 1.3328 mL | |
| 10 mM | 0.0666 mL | 0.3332 mL | 0.6664 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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