Home >> Research Area >>GPCR/G protein>>Bombesin Receptors>> [D-Phe12,Leu14]-Bombesin

[D-Phe12,Leu14]-Bombesin

Bombesin receptor antagonist CAS# 108437-88-3

[D-Phe12,Leu14]-Bombesin

Catalog No. BCC6020----Order now to get a substantial discount!

Product Name & Size Price Stock
[D-Phe12,Leu14]-Bombesin: 5mg $656 In Stock
[D-Phe12,Leu14]-Bombesin: 10mg Please Inquire In Stock
[D-Phe12,Leu14]-Bombesin: 20mg Please Inquire Please Inquire
[D-Phe12,Leu14]-Bombesin: 50mg Please Inquire Please Inquire
[D-Phe12,Leu14]-Bombesin: 100mg Please Inquire Please Inquire
[D-Phe12,Leu14]-Bombesin: 200mg Please Inquire Please Inquire
[D-Phe12,Leu14]-Bombesin: 500mg Please Inquire Please Inquire
[D-Phe12,Leu14]-Bombesin: 1000mg Please Inquire Please Inquire
Related Products

Quality Control of [D-Phe12,Leu14]-Bombesin

Number of papers citing our products

Chemical structure

[D-Phe12,Leu14]-Bombesin

3D structure

Chemical Properties of [D-Phe12,Leu14]-Bombesin

Cas No. 108437-88-3 SDF Download SDF
PubChem ID 16168803 Appearance Powder
Formula C75H114N22O18 M.Wt 1611.8
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 10 mg/ml in water
Sequence XQRLGNQWAVGFLL

(Modifications: X = Glp, Phe-12 = D-Phe, Leu-14 = C-terminal amide)

Chemical Name (2S)-N-[(2S)-1-[[(2S)-1-[[2-[[(2S)-4-amino-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2R)-1-[[(2S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]-2-[[(2S)-5-oxopyrrolidine-2-carbonyl]amino]pentanediamide
SMILES CC(C)CC(C(=O)N)NC(=O)C(CC(C)C)NC(=O)C(CC1=CC=CC=C1)NC(=O)CNC(=O)C(C(C)C)NC(=O)C(C)NC(=O)C(CC2=CNC3=CC=CC=C32)NC(=O)C(CCC(=O)N)NC(=O)C(CC(=O)N)NC(=O)CNC(=O)C(CC(C)C)NC(=O)C(CCCNC(=N)N)NC(=O)C(CCC(=O)N)NC(=O)C4CCC(=O)N4
Standard InChIKey PWGHKRYOBBMXGB-TVXZQRGPSA-N
Standard InChI InChI=1S/C75H114N22O18/c1-37(2)28-50(63(79)104)93-71(112)52(30-39(5)6)95-72(113)53(31-42-16-11-10-12-17-42)88-61(103)36-85-74(115)62(40(7)8)97-64(105)41(9)86-70(111)54(32-43-34-83-45-19-14-13-18-44(43)45)96-69(110)49(22-25-57(77)99)92-73(114)55(33-58(78)100)89-60(102)35-84-65(106)51(29-38(3)4)94-66(107)46(20-15-27-82-75(80)81)90-68(109)48(21-24-56(76)98)91-67(108)47-23-26-59(101)87-47/h10-14,16-19,34,37-41,46-55,62,83H,15,20-33,35-36H2,1-9H3,(H2,76,98)(H2,77,99)(H2,78,100)(H2,79,104)(H,84,106)(H,85,115)(H,86,111)(H,87,101)(H,88,103)(H,89,102)(H,90,109)(H,91,108)(H,92,114)(H,93,112)(H,94,107)(H,95,113)(H,96,110)(H,97,105)(H4,80,81,82)/t41-,46-,47-,48-,49-,50-,51-,52-,53+,54-,55-,62-/m0/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.
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.
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.

Biological Activity of [D-Phe12,Leu14]-Bombesin

DescriptionBombesin receptor antagonist that inhibits bombesin binding to rat brain with an IC50 value of 2 μM. Inhibits amylase release in vitro (IC50 = 4 μM) and attenuates bombesin-mediated suppression of food intake in vivo.

[D-Phe12,Leu14]-Bombesin Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

[D-Phe12,Leu14]-Bombesin Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Organizitions Citing Our Products recently

 
 
 

Calcutta University

University of Minnesota

University of Maryland School of Medicine

University of Illinois at Chicago

The Ohio State University

University of Zurich

Harvard University

Colorado State University

Auburn University

Yale University

Worcester Polytechnic Institute

Washington State University

Stanford University

University of Leipzig

Universidade da Beira Interior

The Institute of Cancer Research

Heidelberg University

University of Amsterdam

University of Auckland
TsingHua University
TsingHua University
The University of Michigan
The University of Michigan
Miami University
Miami University
DRURY University
DRURY University
Jilin University
Jilin University
Fudan University
Fudan University
Wuhan University
Wuhan University
Sun Yat-sen University
Sun Yat-sen University
Universite de Paris
Universite de Paris
Deemed University
Deemed University
Auckland University
Auckland University
The University of Tokyo
The University of Tokyo
Korea University
Korea University
Featured Products
New Products
 

References on [D-Phe12,Leu14]-Bombesin

Conformation studies on bombesin receptor antagonists: 500 MHz NMR and CD characterization of synthetic (D-Phe12, Leu14)-bombesin.[Pubmed:2545203]

Biochem Biophys Res Commun. 1989 Jun 30;161(3):987-93.

The conformation flexibility of the tetradecapeptide hormone bombesin and its synthetic antagonist (DPhe12, Leu14)-bombesin has been studied using nuclear magnetic resonance and circular dichroism techniques. The spectral features observed indicate that the ordered structure present in the C-terminal pentapeptide moiety of native BBS is lost in the (DPhe12, Leu14) analog.

Bombesin receptor antagonists block the effects of exogenous bombesin but not of nutrients on food intake.[Pubmed:9284499]

Physiol Behav. 1997 Oct;62(4):791-8.

The endogenous, meal-contingent release of bombesin (BN)-like peptides is thought to contribute to the termination of a meal. In the following experiments the potency of BN receptor antagonists to attenuate the ability of nutrients to suppress food intake was tested. First, the effectiveness of BN receptor subtype antagonists was verified by testing their ability to block the effects of exogenous BN on food intake. Rats were administered intraperitoneal (i.p.) injections of either saline or 0.1 mg/kg [D-Phe12,Leu14]BN (binds both GRP and NMB receptors), [D-Phe6]BN(6-13) ethyl amide (binds GRP > NMB), and cyclo-SS-octa (BIM-23042; binds NMB > GRP). Five minutes later rats were administered 8 micrograms/kg BN (i.p.) and milk intake was measured. Injections of [D-Phe12,Leu14]BN and [D-Phe6]BN(6-13) ethyl amide reliably attenuated the ability of BN to suppress milk intake whereas BIM-23042 was ineffective. The results show that the antagonists were behaviorally effective and that exogenous BN may exert its effects on food intake primarily through the GRP receptor subtype. Next, the antagonists were administered either 5 min prior to or 5 min after an intragastric nutrient load or no load in both overnight-deprived and nondeprived rats, and milk intake was then measured. Stomach loads reduced intake and this effect was not attenuated by BN receptor antagonists. Finally, rats were allowed to prefeed and the milk was then removed. Rats were then administered a BN receptor antagonist (0.1 and 1.0 mg/kg) or saline either immediately after the prefeed, 10 min later, or 20 min later. Milk diet was then returned and intake was measured. Peripheral injections of the BN receptor antagonist had no effect compared to saline on milk intake. Collectively, the results indicate that the blockade of peripheral Bn peptide receptors is not sufficient to attenuate the safety signals generated by stomach loads or prefeeding.

(D-Phe12) bombesin and substance P analogues function as central bombesin receptor antagonists.[Pubmed:2463692]

Synapse. 1988;2(3):282-7.

The potency of synthetic bombesin (BN) analogues with D-Phe12 substitutions and substance P analogues was investigated in the rat CNS. (D-Phe12,Leu14)BN, (D-Phe12)BN and (Tyr4,D-Phe12)BN inhibited binding to rat brain slices with IC50 values of approximately 2 microM. Similarly, spantide inhibited binding to rat brain slices with an IC50 value of 1.5 microM. Spantide inhibited specific (125I-Tyr4)BN binding as a result of decreased rate of association, whereas the rate of dissociation was unaffected. Neither the (D-Phe12)BN analogues nor the substance P analogues inhibited specific binding of 125I-VIP to rat brain slices. Central administration of BN (0.5 micrograms) induced grooming and suppressed feeding and resting. (Tyr4, D-Phe12)BN (5 micrograms) antagonized the behavioral effects of BN. Although spantide (2 micrograms) also antagonized many of the BN effects, it had intrinsic effects and hence the behavioral antagonism was not specific. These data suggest that although both (D-Phe12)BN and substance P analogues may function as central BN receptor antagonists, the (D-Phe12)BN analogues may be functionally the more useful class of antagonists.

[D-Phe12]bombesin analogues: a new class of bombesin receptor antagonists.[Pubmed:2435173]

Am J Physiol. 1987 Mar;252(3 Pt 1):G439-42.

Previous attempts to develop analogues of bombesin that function as specific receptor antagonists have been unsuccessful. Alteration of the histidine in luteinizing hormone releasing factor has resulted in analogues that function as competitive antagonists. In the present study we have used a similar strategy and altered the histidine in bombesin. [D-Phe12]bombesin, [D-Phe12,Leu14]bombesin, and [Tyr4,D-Phe12]bombesin did not stimulate amylase release from guinea pig pancreatic acini when present alone, but each analogue inhibited bombesin-stimulated secretion. For each analogue, detectable inhibition occurred at 1 microM and half-maximal inhibition at 4 microM. Each analogue inhibited amylase release by bombesin and other agonists that stimulate secretion by interacting with bombesin receptors. The analogues of bombesin did not alter stimulation by substance P or other agonists that interact with other receptors. The inhibition of the action of bombesin was competitive with Schild plots having slopes of 1.0. Each analogue also inhibited binding of 125I-labeled [Tyr4]bombesin but not 125I-labeled substance P. These results demonstrate that [D-Phe12] analogues of bombesin function as bombesin receptor antagonists and are the only bombesin receptor antagonists that interact only with the bombesin receptor. Because of their specificity, these analogues may prove useful for defining the role of bombesin in various physiological or pathological processes.

Keywords:

[D-Phe12,Leu14]-Bombesin,108437-88-3,Natural Products,Bombesin Receptors, buy [D-Phe12,Leu14]-Bombesin , [D-Phe12,Leu14]-Bombesin supplier , purchase [D-Phe12,Leu14]-Bombesin , [D-Phe12,Leu14]-Bombesin cost , [D-Phe12,Leu14]-Bombesin manufacturer , order [D-Phe12,Leu14]-Bombesin , high purity [D-Phe12,Leu14]-Bombesin

Online Inquiry for:

      Fill out the information below

      • Size:Qty: - +

      * Required Fields

                                      Result: