Elabela(19-32)

Elabela(19-32) is an active fragment of ELABELA (ELA) that binds to apelin receptor (APJ). Elabela(19-32) activates the Gαi1 and β-arrestin-2 signaling pathways with EC50s of 8.6 nM and 166 nM. Elabela(19-32) induces receptor internalization and reduces arterial pressure, exerts positive inotropic effects on the heart.

Product information

CAS Number: 1886973-05-2

Molecular Weight: 1707.03

Formula: C75H119N25O17S2

Chemical Name: (2S)-1-[(2S)-2-{[(2S)-1-[(2S)-2-[(2S)-5-[(diaminomethylidene)amino]-2-[(2S)-2-[(2S)-2-[(2S)-2-{[(2S)-1-[(2S)-2-[(2R)-2-[(2S)-5-[(diaminomethylidene)amino]-2-[(2S)-5-[(diaminomethylidene)amino]-2-{[(2S)-5-oxopyrrolidin-2-yl]formamido}pentanamido]pentanamido]-3-sulfanylpropanamido]-4-(methylsulfanyl)butanoyl]pyrrolidin-2-yl]formamido}-4-methylpentanamido]-3-(1H-imidazol-5-yl)propanamido]-3-hydroxypropanamido]pentanamido]-3-methylbutanoyl]pyrrolidin-2-yl]formamido}-3-phenylpropanoyl]pyrrolidine-2-carboxylic acid

Smiles: CC(C)[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC1=CN=CN1)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCSC)NC(=O)[C@H](CS)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N1CCC[C@H]1C(O)=O

InChiKey: LKYSPGTYQNANFL-GYVBEWGNSA-N

InChi: InChI=1S/C75H119N25O17S2/c1-40(2)33-49(93-67(111)54-20-12-29-98(54)69(113)48(25-32-119-5)91-66(110)53(38-118)96-60(104)45(18-10-27-84-74(78)79)88-59(103)44(17-9-26-83-73(76)77)89-61(105)47-23-24-57(102)87-47)63(107)92-50(35-43-36-82-39-86-43)64(108)95-52(37-101)65(109)90-46(19-11-28-85-75(80)81)62(106)97-58(41(3)4)71(115)99-30-13-21-55(99)68(112)94-51(34-42-15-7-6-8-16-42)70(114)100-31-14-22-56(100)72(116)117/h6-8,15-16,36,39-41,44-56,58,101,118H,9-14,17-35,37-38H2,1-5H3,(H,82,86)(H,87,102)(H,88,103)(H,89,105)(H,90,109)(H,91,110)(H,92,107)(H,93,111)(H,94,112)(H,95,108)(H,96,104)(H,97,106)(H,116,117)(H4,76,77,83)(H4,78,79,84)(H4,80,81,85)/t44-,45-,46-,47-,48-,49-,50-,51-,52-,53-,54-,55-,56-,58-/m0/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: H2O : 100 mg/mL (58.58 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

Elabela(19-32) (analogue 3) has a Ki of 0.93 nM for binding of radioligand apelin-13[Glp65, Nle75, Tyr77][125I]. Elabela(19-32) has an EC50 of 36 nM in HEK293 cells transiently expressing the HA-hAPJ receptor. Elabela(19-32) is slightly less potent than apelin-13 and ELA to elicit receptor internalization. Elabela(19-32) (0.001 to 0.3 nM) has an EC50 of 1.5 pM in inducing changes in left ventricular developed pressure (LVDP) on the Langendorff perfused isolated rat heart.

In Vivo:

Elabela(19-32) (analogue 3) is rapidly metabolized in rat plasma (t1/2<2 min).

Products are for research use only. Not for human use.