| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
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Purity: = 99.58%
| Targets |
vasopressin V1 receptor
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| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Following a 1 mg IV injection of terlipressin acetate in patients with HRS-1, the median Cmax, AUC24h and Cave of terlipressin at steady-state were 70.5 ng/mL, 123 ng × hr/mL and 14.2 ng/mL, respectively. The median Cmax, AUC24h and Cave of lypressin were 1.2 ng/mL, 11.2 ng × hr/mL and 0.5 ng/mL, respectively. Terlipressin and lypressin exhibit linear pharmacokinetics in healthy subjects. Plasma concentrations of terlipressin demonstrate proportional increases with the dose administered. Less than 1% of terlipressin and <0.1% of lysine-vasopressin is excreted in urine in healthy subjects. The volume of distribution of terlipressin was 6.3 L and 1370 L for lysine-vasopressin. The clearance of terlipressin was 27.4 L/hr and 318 L/hr for lysine-vasopressin. Clearance of terlipressin in HRS-1 patients increased with body weight, while body weight had no effect on the clearance of lysine-vasopressin. Metabolism / Metabolites The N-terminal glycyl residues of terlipressin is cleaved by various tissue peptidases to release its pharmacologically active metabolite, [lypressin] or lysine-vasopressin. Once formed, lypressin is undergoes various peptidase-mediated metabolic pathways in body tissues. Terlipressin is not metabolized in the blood or plasma. Due to the ubiquitous nature of peptidases in body tissues, it is unlikely that the metabolism of terlipressin will be affected by disease state or other drugs. Biological Half-Life The terminal half-life of terlipressin was 0.9 hours and 3.0 hours for lysine-vasopressin. |
| References |
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| Additional Infomation |
Pharmacodynamics
Terlipressin mimics the biological effects of endogenous vasopressin, but it displays increased selectivity for the V1 receptor and a longer half-life than vasopressin. These pharmacokinetic and molecular properties of terlipressin give it several advantages, such as the prevention of rebound hypotension when the drug is stopped and convenience in patients with limited intravenous access. Terlipressin increases arterial pressure (diastolic, systolic, and mean) and decreases heart rate in patients with hepatorenal syndrome type 1 (HRS-1). After the administration of a single 0.85 mg dose of terlipressin in patients with HRS-1, cardiovascular effects were observed within five minutes after dosing and were maintained for at least six hours after dosing. The maximum change in blood pressure and heart rate occurred at 1.2 to two hours post-dose. |
| Molecular Formula |
C54H78N16O17S2
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|---|---|
| Molecular Weight |
1287.433
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| Exact Mass |
1346.538
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| Elemental Analysis |
C, 50.38; H, 6.11; N, 17.41; O, 21.13; S, 4.98
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| CAS # |
914453-96-6
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| Related CAS # |
Terlipressin diacetate; 1884420-36-3; Terlipressin; 14636-12-5
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| PubChem CID |
72081
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| Appearance |
White to off-white solid powder
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| LogP |
-5.8
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| Hydrogen Bond Donor Count |
16
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| Hydrogen Bond Acceptor Count |
19
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| Rotatable Bond Count |
25
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| Heavy Atom Count |
85
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| Complexity |
2380
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| Defined Atom Stereocenter Count |
8
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| SMILES |
S1C[C@@H](C(N2CCC[C@H]2C(N[C@H](C(NCC(N)=O)=O)CCCCN)=O)=O)NC([C@H](CC(N)=O)NC([C@H](CCC(N)=O)NC([C@H](CC2C=CC=CC=2)NC([C@H](CC2C=CC(=CC=2)O)NC([C@H](CS1)NC(CNC(CNC(CN)=O)=O)=O)=O)=O)=O)=O)=O.OC(C)=O
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| InChi Key |
BYDVFOPTAIPAGA-LCGYVTRFSA-N
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| InChi Code |
InChI=1S/C52H74N16O15S2.C2H4O2/c53-17-5-4-9-31(45(76)60-23-41(57)72)63-51(82)38-10-6-18-68(38)52(83)37-27-85-84-26-36(61-44(75)25-59-43(74)24-58-42(73)22-54)50(81)65-34(20-29-11-13-30(69)14-12-29)48(79)64-33(19-28-7-2-1-3-8-28)47(78)62-32(15-16-39(55)70)46(77)66-35(21-40(56)71)49(80)67-37;1-2(3)4/h1-3,7-8,11-14,31-38,69H,4-6,9-10,15-27,53-54H2,(H2,55,70)(H2,56,71)(H2,57,72)(H,58,73)(H,59,74)(H,60,76)(H,61,75)(H,62,78)(H,63,82)(H,64,79)(H,65,81)(H,66,77)(H,67,80);1H3,(H,3,4)/t31-,32-,33-,34-,35-,36-,37-,38-;/m0./s1
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| Chemical Name |
acetic acid;(2S)-1-[(4R,7S,10S,13S,16S,19R)-19-[[2-[[2-[(2-aminoacetyl)amino]acetyl]amino]acetyl]amino]-7-(2-amino-2-oxoethyl)-10-(3-amino-3-oxopropyl)-13-benzyl-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]-N-[(2S)-6-amino-1-[(2-amino-2-oxoethyl)amino]-1-oxohexan-2-yl]pyrrolidine-2-carboxamide
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| Synonyms |
Gly-Gly-Gly-8-Lys-vasopressin; TGLVP; triglycyl lysine vasopressin; Terlipressin; Terlipressin acetate; trade names: Glypressin; Teripress
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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 |
| 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) |
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
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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 | 0.7767 mL | 3.8837 mL | 7.7674 mL | |
| 5 mM | 0.1553 mL | 0.7767 mL | 1.5535 mL | |
| 10 mM | 0.0777 mL | 0.3884 mL | 0.7767 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.
Treatment of hepatorenal syndrome with terlipressin infusion adjusted to hemodynamic response
CTID: null
Phase: Phase 4 Status: Completed
Date: 2012-02-08
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