Tabimorelin hemifumaratePotent, orally active ghrelin receptor agonist CAS# 242143-80-2 |
- FLAG tag Peptide
Catalog No.:BCC2562
CAS No.:98849-88-8
Quality Control & MSDS
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Chemical structure
3D structure
| Cas No. | 242143-80-2 | SDF | Download SDF |
| PubChem ID | 11981159 | Appearance | Powder |
| Formula | C68H84N8O10 | M.Wt | 1173.4 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | NN 703 | ||
| Solubility | Soluble to 10 mM in water with gentle warming and to 100 mM in DMSO | ||
| Chemical Name | (E)-5-amino-N,5-dimethyl-N-[(2R)-1-[methyl-[(2R)-1-(methylamino)-1-oxo-3-phenylpropan-2-yl]amino]-3-naphthalen-2-yl-1-oxopropan-2-yl]hex-2-enamide;(E)-but-2-enedioic acid | ||
| SMILES | CC(C)(CC=CC(=O)N(C)C(CC1=CC2=CC=CC=C2C=C1)C(=O)N(C)C(CC3=CC=CC=C3)C(=O)NC)N.CC(C)(CC=CC(=O)N(C)C(CC1=CC2=CC=CC=C2C=C1)C(=O)N(C)C(CC3=CC=CC=C3)C(=O)NC)N.C(=CC(=O)O)C(=O)O | ||
| Standard InChIKey | YQDJPWXYLLPOPW-LWTUVRFUSA-N | ||
| Standard InChI | InChI=1S/2C32H40N4O3.C4H4O4/c2*1-32(2,33)19-11-16-29(37)35(4)28(22-24-17-18-25-14-9-10-15-26(25)20-24)31(39)36(5)27(30(38)34-3)21-23-12-7-6-8-13-23;5-3(6)1-2-4(7)8/h2*6-18,20,27-28H,19,21-22,33H2,1-5H3,(H,34,38);1-2H,(H,5,6)(H,7,8)/b2*16-11+;2-1+/t2*27-,28-;/m11./s1 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Potent, orally active ghrelin receptor (GHS-R1a) agonist (Ki = 50 nM at human recombinant GHS-R1a). Stimulates GH release from rat pituitary cells with an EC50 value of 2.7 nM. Induces hyperphagia and adiposity in lean rats, but not in leptin signaling-deficient ZDF rats. |
Tabimorelin hemifumarate Dilution Calculator
Tabimorelin hemifumarate Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 0.8522 mL | 4.2611 mL | 8.5222 mL | 17.0445 mL | 21.3056 mL |
| 5 mM | 0.1704 mL | 0.8522 mL | 1.7044 mL | 3.4089 mL | 4.2611 mL |
| 10 mM | 0.0852 mL | 0.4261 mL | 0.8522 mL | 1.7044 mL | 2.1306 mL |
| 50 mM | 0.017 mL | 0.0852 mL | 0.1704 mL | 0.3409 mL | 0.4261 mL |
| 100 mM | 0.0085 mL | 0.0426 mL | 0.0852 mL | 0.1704 mL | 0.2131 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Pharmacological characterisation of a new oral GH secretagogue, NN703.[Pubmed:10427162]
Eur J Endocrinol. 1999 Aug;141(2):180-9.
NN703 is a novel orally active GH secretagogue (GHS) derived from ipamorelin. NN703 stimulates GH release from rat pituitary cells in a dose-dependent manner with a potency and efficacy similar to that of GHRP-6. The effect is inhibited by known GHS antagonists, but not by a GH-releasing hormone antagonist. Binding of (35)S-MK677 to the human type 1A GHS receptor (GHS-R 1A) stably expressed on BHK cells was inhibited by GHRP-6 and MK677 as expected. NN703 was also able to inhibit the binding of (35)S-MK677. However, the observed K(i) value was lower than expected, as based on the observed potencies regarding GH release from rat pituitary cells. Similarly, the effect of NN703 on the GHS-R 1A-induced inositol phosphate turnover in these cells showed a lower potency, when compared with GHRP-6 and MK677, than that observed in rat pituitary cells. The effect of i.v. administration of NN703 on GH and cortisol release was studied in swine. The potency and efficacy of NN703 on GH release were determined to be 155+/-23 nmol/kg and 91+/-7 ng GH/ml plasma respectively. A 50% increase of cortisol, compared with basal levels, was observed for all the tested doses of NN703, but no dose-dependency was shown. The effect of NN703 on GH release after i. v. and oral dosing in beagle dogs was studied. NN703 dose-dependently increased the GH release after oral administration. At the highest dose (20 micromol/kg), a 35-fold increase in peak GH concentration was observed (49.5+/-17.8 ng/ml, mean+/-s.e.m.). After a single i.v. dose of 1 micromol/kg the peak GH plasma concentration was elevated to 38.5+/-19.6 ng/ml (mean+/-s.e.m.) approximately 30 min after dosing and returned to basal level after 360 min. The oral bioavailability was 30%. The plasma half-life of NN703 was 4.1+/-0.4 h. A long-term biological effect of NN703 was demonstrated in a rat study, where the body weight gain was measured during a 14-day once daily oral challenge with 100 micromol/kg. The body weight gain was significantly increased after 14 days as compared with a vehicle-treated group. In summary, we here describe an orally active and GH specific secretagogue, NN703. This compound acts through a similar mechanism as GHRP-6, but has a different receptor pharmacology. NN703 induced GH release in both swine and dogs after i.v. and/or p.o. administration, had a high degree of GH specificity in swine and significantly increased the body weight gain in rats.
