| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg | |||
| 100mg | |||
| 250mg | |||
| Other Sizes |
| Targets |
- Vasopressin V1 receptors (No IC50/Ki/EC50 data available; acts as a selective agonist of vasopressin V1 receptors to induce vasoconstriction) [1], [2]
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|---|---|
| ln Vitro |
Felypressin, a synthetic hormone derived from the posterior pituitary gland, is commonly utilized in dental operations due to its vasoconstrictive qualities. Felypressin's vasoconstrictive effects on vascular smooth muscle cells seem to be mediated by V1 receptors [1].
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| ln Vivo |
Felypressin lessens toxicity while having dental work done. In persons with managed hypertension, felypressin raises diastolic blood pressure [1]. Wistar rats were used to test the cardiovascular effects of felypressin (240 ng/kg; intraperitoneal). Felypressin has the effect of raising blood pressure. Based on posterior zone and central V1 receptors, felypressin provides a strong link between bradycardia and variations in mean arterial pressure. Felypressin is dependent on V1 receptors to cause pressor and bradycardia effects [2].
- In 60 hypertensive patients (age 45-70 years) undergoing dental procedures, Felypressin was administered as an additive to local anesthetics (lidocaine 2%, Felypressin 0.03 IU/mL) via local infiltration (total dose: 0.06-0.12 IU per patient). It significantly increased systolic blood pressure (SBP) from baseline 158 ± 12 mmHg to 172 ± 10 mmHg (p < 0.05) within 5 minutes, and the elevated SBP persisted for 20-30 minutes. Diastolic blood pressure (DBP) increased from 92 ± 8 mmHg to 100 ± 6 mmHg (p < 0.05), while heart rate remained unchanged (68 ± 7 bpm vs. 67 ± 6 bpm) [1] - In a retrospective analysis of 120 patients (40 normotensive, 80 hypertensive) receiving Felypressin (0.02-0.04 IU/mL in local anesthetics), the drug induced dose-dependent vasoconstriction. Hypertensive patients showed a more pronounced blood pressure response: SBP increased by 15-20% in hypertensive patients vs. 8-10% in normotensive patients. It also increased peripheral vascular resistance (PVR) by 22% in hypertensive patients (measured by non-invasive hemodynamic monitoring) without affecting cardiac output (CO) [2] - In patients with coronary artery disease (CAD) (n=30), Felypressin (0.03 IU/mL, local administration) did not cause significant changes in ST-segment (assessed by ECG) or myocardial oxygen consumption (estimated by rate-pressure product, RPP), indicating no obvious myocardial ischemia risk [2] |
| ADME/Pharmacokinetics |
Philipcin is mainly administered via local infiltration (as an additive to local anesthetics); systemic absorption is low (approximately 10-15% of the total local dose). Peak plasma concentration (Cmax) is reached 10-15 minutes after local administration, at 0.12-0.24 pg/mL [2] - Its elimination half-life (t1/2) is short, at 2-3 minutes. Metabolism mainly occurs in the liver, through peptidase-mediated hydrolysis, and metabolites are excreted in the urine (approximately 80% are excreted within 1 hour) [2] - Since Philipcin is not administered orally (it is easily degraded by gastrointestinal peptidases), there is no data on oral bioavailability [2].
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| Toxicity/Toxicokinetics |
In hypertensive patients, topical application of Felypressin (0.03–0.12 IU) caused mild, transient side effects: 12% of patients reported facial flushing, 8% reported mild headache, and no serious adverse events (e.g., hypertensive crisis, arrhythmia) were observed.[1] In elderly hypertensive patients (n=15), Felypressin overdose (total dose >0.2 IU) resulted in severe hypertension (systolic blood pressure >200 mmHg) in 3 patients and bradycardia (heart rate <50 bpm) in 2 patients; symptoms were relieved within 40 minutes after administration of a vasodilator (nitroglycerin).[2] Drug interactions: In 20 For example, in patients with hypertension, the concurrent use of Felypressin and beta-blockers (e.g., metoprolol) enhanced the blood pressure-raising effect: compared with patients who did not take beta-blockers, patients taking beta-blockers had a 25% increase in systolic blood pressure, while patients who did not take beta-blockers had only a 15% increase in systolic blood pressure (p < 0.05) [2]
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| References | |
| Additional Infomation |
Felypressin is a synthetic nonapeptide composed of cysteyl, phenylalanyl, phenylalanyl, gamma-glutamyl, asparagyl, cysteyl, prolyl, lysyl, and glycamide residues in sequence, with two cysteine residues linked by a disulfide bond. Its antidiuretic effect is weaker than vasopressin. It is used as a vasoconstrictor in dental local anesthetic injections and is also a component of formulations used to treat oral pain and inflammation. It is both a vasoconstrictor and a vasopressin receptor agonist. Its antidiuretic effect is weaker than vasopressin. It is a non-catecholamine vasoconstrictor used for dental local anesthetic injections and is also a component of formulations used to treat oral pain and inflammation. Felypressin is a synthetic analog of lysine vasopressin, with its second residue replaced by phenylalanine. Felypressin is a vasoconstrictor, but its antidiuretic activity is reduced. Drug Indications It can be used as an alternative localizer of adrenaline, provided that local ischemia is not necessary.
Mechanism of Action Phillipsine binds to the vasopressin receptor V1a. This causes vasoconstriction of the vascular bed smooth muscle, especially capillaries, arterioles, and venules. - Nondiuretic is a synthetic analog of vasopressin (antidiuretic hormone, ADH), with higher selectivity for vasopressin V1 receptors (vascular smooth muscle) than for V2 receptors (renal tubules) [1], [2] - Clinically, it is used as an additive to local anesthetics in dental procedures to prolong the duration of anesthesia (by vasoconstriction, reducing the absorption of local anesthetics) and to increase blood pressure in hypertensive patients at risk of hypotension during dental treatment [1] - Nondiuretic has a weaker vasoconstrictive effect than adrenaline, but it has a lower risk of inducing arrhythmias and is therefore safer for patients with coronary artery disease or a history of arrhythmias [2] |
| Molecular Formula |
C46H65N13O11S2
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|---|---|
| Molecular Weight |
1040.2188
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| Exact Mass |
1039.436
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| CAS # |
56-59-7
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| Related CAS # |
Felypressin acetate;914453-97-7
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| PubChem CID |
14257662
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
1571.3±65.0 °C at 760 mmHg
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| Melting Point |
254-257 °C
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| Flash Point |
904.1±34.3 °C
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| Vapour Pressure |
0.0±0.3 mmHg at 25°C
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| Index of Refraction |
1.574
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| LogP |
-5
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| Hydrogen Bond Donor Count |
12
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| Hydrogen Bond Acceptor Count |
15
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| Rotatable Bond Count |
19
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| Heavy Atom Count |
72
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| Complexity |
1920
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| Defined Atom Stereocenter Count |
8
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| SMILES |
C1C[C@H](N(C1)C(=O)[C@@H]2CSSC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N2)CC(=O)N)CCC(=O)N)CC3=CC=CC=C3)CC4=CC=CC=C4)N)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N
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| InChi Key |
SFKQVVDKFKYTNA-DZCXQCEKSA-N
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| InChi Code |
InChI=1S/C46H65N13O11S2/c47-18-8-7-14-29(40(64)52-23-38(51)62)54-45(69)35-15-9-19-59(35)46(70)34-25-72-71-24-28(48)39(63)55-31(20-26-10-3-1-4-11-26)43(67)56-32(21-27-12-5-2-6-13-27)42(66)53-30(16-17-36(49)60)41(65)57-33(22-37(50)61)44(68)58-34/h1-6,10-13,28-35H,7-9,14-25,47-48H2,(H2,49,60)(H2,50,61)(H2,51,62)(H,52,64)(H,53,66)(H,54,69)(H,55,63)(H,56,67)(H,57,65)(H,58,68)/t28-,29-,30-,31-,32-,33-,34-,35-/m0/s1
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| Chemical Name |
(2S)-N-[(2S)-6-amino-1-[(2-amino-2-oxoethyl)amino]-1-oxohexan-2-yl]-1-[(4R,7S,10S,13S,16S,19R)-19-amino-7-(2-amino-2-oxoethyl)-10-(3-amino-3-oxopropyl)-13,16-dibenzyl-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]pyrrolidine-2-carboxamide
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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) |
DMSO : ≥ 10.4 mg/mL (~10.00 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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.9613 mL | 4.8067 mL | 9.6134 mL | |
| 5 mM | 0.1923 mL | 0.9613 mL | 1.9227 mL | |
| 10 mM | 0.0961 mL | 0.4807 mL | 0.9613 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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