- Shanghai Nianxing Industrial Co., Ltd
- China
- Product Name: IRL-1620?
- Price:
- Purity: 98.0%
- Stocking Period: 10 Day
- Contact: Yang
- DC Chemicals Limited
- China
- Product Name: Irl-1620
- Price: ￥Inquiry/100mg ￥Inquiry/250mg ￥Inquiry/1g
- Purity: 98.0%
- Stocking Period: 10 Day
- Contact: Tony Cao
- Taiwan Oyi peptide Co. Ltd
- China
- Product Name: IRL-1620 TFA
- Price: $Inquiry/1mg $Inquiry/100kg
- Purity: 98.0%
- Stocking Period: 1 Day
- Contact: Vinnie
142569-99-1
142569-99-1 structure
- Name: IRL-1620 TFA
- Chemical Name: Succinyl-(glu(9),ala(11,15))-endothelin-1 (8-21)
- CAS Number: 142569-99-1
- Molecular Formula: C86H117N17O27
- Molecular Weight: 1820.947
- Catalog: Peptides
- Create Date: 2019-01-08 13:14:47
- Modify Date: 2024-01-08 17:28:02
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IRL-1620 is a potent and selective endothelin receptor type B (ETB) agonist with a Ki of 16 pM.
| Name | Succinyl-(glu(9),ala(11,15))-endothelin-1 (8-21) |
|---|---|
| Synonyms |
N-(3-Carboxypropanoyl)-L-α-aspartyl-L-α-glutamyl-L-α-glutamyl-L-alanyl-L-valyl-L-tyrosyl-L-phenylalanyl-L-alanyl-L-histidyl-L-leucyl-L-α-aspartyl-L-isoleucyl-L-isoleucyl-L-tryptophan
Irl-1620 N-Succinyl-[Glu9,Ala11,15]-Endothelin 1 fragment 8-21 L-Tryptophan, N-(3-carboxy-1-oxopropyl)-L-α-aspartyl-L-α-glutamyl-L-α-glutamyl-L-alanyl-L-valyl-L-tyrosyl-L-phenylalanyl-L-alanyl-L-histidyl-L-leucyl-L-α-aspartyl-L-isoleucyl-L-isoleuc 
yl- MFCD00214284 |
| Description | IRL-1620 is a potent and selective endothelin receptor type B (ETB) agonist with a Ki of 16 pM. |
|---|---|
| Related Catalog | |
| Target |
IC50: 16 pM (Endothelin receptor B), 19 μM (Endothelin receptor A)[1] |
| In Vitro | IRL 1620 is the most potent and specific ligand for the ETB receptor (KiETA/ KiETB=120,000) as judged by the Ki values for ETA (19 μM) and ETB (16 PM) receptors. IRL 1620 is 60 times more selective for the ETB receptor than ET-3 (KiETA/ KiETB=1,900)[1]. |
| In Vivo | IRL 1620 (1-100 nM) induces contractions of the guinea pig trachea. The effective concentration that produces 30 % of 60 mM KCI-induced contraction is estimated to be 28 nM for IRL 1620. In rat aorta, IRL 1620 (1-100 nM) increases cytosolic Ca2+ in the vascular endothelium ([Ca]E) with little effect on resting muscle tone, and relaxes the norepinephrine-stimulated tone with an increase in [Ca]E[1]. IRL-1620 improves both acquisition (learning) and retention (memory) on the water maze task and enhances angiogenic and neurogenic remodeling. Rats treated with IRL-1620 significantly reduces the cognitive impairment induced by Aβ. IRL-1620 treatment enhances the number of blood vessels labeled with VEGF compared to vehicle treatment[2]. IRL-1620, restores analgesic tolerance to morphine and oxycodone, but it does not affect morphine and oxycodone induced decrease in NGF/PI3K expression. IRL-1620 attenuates opioid tolerance without the involvement of NGF/PI3K pathway[3]. |
| Kinase Assay | The plasma membrane of porcine lung (2 ug of protein) is incubated at 37°C for 1 hr with 30 pM [125I]ET-1 or 10 pM [125I]ET-3 in the absence or presence of various amounts of nonlabeled ligands (IRL-1620) in a total volume of 1 mL of assay buffer. After the incubation, unbound [125I]ETs are separated and radioactivity in the membrane pellet is measured in an autogamma counter[1]. |
| Animal Admin | Rats: Specific ETB receptor agonist, IRL-1620 (5 μg/kg) and specific ETB receptor antagonist, BQ788 (1 mg/kg) are administered intravenously (i.v.) on day 8. IRL-1620 is administered on day 8 three times at a dose of 5 μg/kg, i.v. at 2-h intervals between each injection[2]. Mice: Tolerance to morphine is induced using a 3-day cumulative dosing regimen. Morphine treatment schedule consisted of twice-daily s.c. injections of morphine for three days given at (i) 30 mg/kg (a.m.) and 45 mg/kg (p.m.) on day 1; (ii) 60 mg/kg (a.m.) and 90 mg/kg (p.m.) on day 2; and (iii) 120 mg/kg twice (a.m. and p.m.) on day 3. The IRL-1620 treatment schedule consists of three times-daily injections of IRL-1620 for two days given at 5 μg/kg, i.v. spaced apart every 2 h on days 1 and 3. At the end of the treatment schedule, a challenge dose of morphine (5 mg/kg, s.c.) is administered on day 4 to assess tolerance[3]. |
| References |
| Density | 1.3±0.1 g/cm3 |
|---|---|
| Boiling Point | 2096.6±65.0 °C at 760 mmHg |
| Molecular Formula | C86H117N17O27 |
| Molecular Weight | 1820.947 |
| Flash Point | 1221.8±34.3 °C |
| Exact Mass | 1819.830444 |
| PSA | 695.90000 |
| LogP | 4.15 |
| Vapour Pressure | 0.0±0.3 mmHg at 25°C |
| Index of Refraction | 1.593 |
| Storage condition | 2-8℃ |