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| Targets |
OGP targets the OGP receptor (OGPR), a G protein-coupled receptor expressed on osteoblast lineage cells. The active portion of OGP, the OGP(10-14) region (Tyr-Gly-Phe-Gly-Gly), is cleaved from the full-length 14-mer peptide and binds to the OGP receptor. Upon ligand binding, the receptor activates multiple signaling pathways including the MAP kinase (ERK1/2) pathway, the Src kinase pathway, and the RhoA pathway. These signaling cascades regulate the proliferation, differentiation, and matrix mineralization of osteoblasts, the cells responsible for bone formation. The OGP receptor is also known as the CXC chemokine receptor type 4 (CXCR4) in some studies. OGP's effects are mediated through these signaling pathways, which coordinate the osteogenic response to bone injury and regulate bone remodeling.
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| ln Vitro |
The osteoblast lineage's cell division, proliferation, and matrix mineralization are all regulated by osteogenic growth peptide (OGP). After being separated from the peptide, the OGP(10–14) region, which is the active portion of OGP, binds to the OGP receptor and initiates the Src, RhoA, and MAP kinase pathways [1]. Osteogenic growth peptide (OGP) is a naturally occurring molecule with a highly conserved 14 amino acid motif (NH2-ALKRQGRTLYGFGG-OH) in its sequence. Its fundamental structure is identical to the C-terminus of histone H4. This peptide was extracted from blood during bone marrow regenerative ablation and used in osteogenic remodeling. It has been demonstrated that osteogenic growth peptide (OGP) and its C-terminal pentapeptide OGP (10–14) promote osteoblast lineage cell proliferation, differentiation, alkaline phosphatase activity, and matrix mineralization [2].
OGP demonstrates potent in vitro activity in osteoblast lineage cells. The peptide regulates the proliferation, differentiation, and matrix mineralization of osteoblast lineage cells in a dose-dependent manner. In cell culture studies, OGP stimulates osteoblast proliferation and increases the expression of osteogenic markers such as alkaline phosphatase, osteocalcin, and type I collagen. The active OGP(10-14) fragment retains the full biological activity of the parent peptide. The peptide's effects are mediated through the OGP receptor and downstream signaling pathways including MAP kinase, Src, and RhoA. OGP has been shown to enhance the formation of mineralized bone nodules in osteoblast cultures. The peptide's activity has been characterized in multiple in vitro systems using primary osteoblast cultures and osteoblast cell lines such as MC3T3-E1 and SaOS-2. |
| ln Vivo |
In vivo, OGP has demonstrated osteogenic activity in animal models of bone injury and osteoporosis. As a key factor in the systemic osteogenic response to local bone marrow injury, OGP promotes bone formation and regeneration. In animal models, administration of OGP has been shown to increase bone mineral density, enhance fracture healing, and stimulate bone formation. The peptide's effects are mediated through the OGP receptor and downstream signaling pathways in osteoblasts. OGP has been studied in models of osteoporosis, where it has demonstrated potential for stimulating bone formation and reducing bone loss. The peptide's naturally occurring presence in serum at micromolar concentrations suggests a physiological role in bone homeostasis. In vivo studies have confirmed the osteogenic activity of both the full-length OGP peptide and the active OGP(10-14) fragment.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for OGP are not standard, as the peptide is a receptor agonist rather than an enzyme inhibitor. Receptor binding assays can be performed using radiolabeled OGP or OGP(10-14) to study binding to the OGP receptor (OGPR). Membranes from cells expressing the OGP receptor are incubated with varying concentrations of labeled peptide and unlabeled competitor to determine binding affinity (Kd) and competitive binding (IC50). Alternatively, cell-based signaling assays can measure receptor activation by assessing downstream signaling pathways. For example, phosphorylation of ERK1/2, Src, or RhoA activation can be measured by Western blot or immunoassay following OGP treatment. The active OGP(10-14) fragment is typically used in these assays as it retains full biological activity. Assays are performed in appropriate buffer systems with controls for non-specific binding and signaling.
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| Cell Assay |
In vitro cellular assays for OGP are performed using osteoblast lineage cells such as primary osteoblasts, MC3T3-E1 cells, or SaOS-2 cells. Cells are cultured in appropriate medium and treated with OGP or OGP(10-14) at concentrations ranging from picomolar to micromolar for various time periods. Cell proliferation is assessed using assays such as BrdU incorporation, MTT, or direct cell counting. Differentiation is evaluated by measuring alkaline phosphatase activity, osteocalcin production, and matrix mineralization (alizarin red or von Kossa staining). Gene expression is analyzed by qRT-PCR for osteogenic markers including Runx2, osteocalcin, alkaline phosphatase, and type I collagen. Signaling pathway activation is assessed by Western blot for phosphorylated ERK1/2, Src, and RhoA. Cytotoxicity is assessed in parallel using standard viability assays.
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| Animal Protocol |
In vivo animal studies for OGP are conducted using rodent models of bone injury, fracture healing, or osteoporosis. Typically, 6-8 week old male or female rats or mice are used. In bone injury models, a critical-sized bone defect is created in the femur or tibia, and OGP or vehicle is administered locally or systemically. In fracture healing models, a standardized fracture is created, and healing is assessed by X-ray, micro-CT, and biomechanical testing. In osteoporosis models, ovariectomized animals are used to simulate postmenopausal bone loss, and OGP is administered to assess its ability to prevent bone loss or stimulate bone formation. Bone mineral density is measured by DXA or micro-CT, and bone histomorphometry is performed on undecalcified bone sections. Serum markers of bone formation (P1NP) and resorption (CTX-1) are measured. Body weight and clinical observations are monitored as safety indicators.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of OGP are characteristic of a peptide therapeutic. OGP is a naturally occurring peptide found in serum at micromolar concentrations. As a peptide, OGP is susceptible to proteolytic degradation and has a relatively short half-life in circulation. The peptide is typically administered by injection (subcutaneous, intraperitoneal, or intravenous) due to poor oral bioavailability. The active OGP(10-14) fragment has been studied as a potential therapeutic agent, with improved stability and activity compared to the full-length peptide. OGP has a molecular weight of approximately 1.5 kDa and consists of 14 amino acids. Comprehensive pharmacokinetic parameters including half-life, volume of distribution, clearance, and bioavailability have been characterized in preclinical studies. The peptide's stability in solution is limited, and fresh solutions are typically prepared for experiments.
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| Toxicity/Toxicokinetics |
OGP is a naturally occurring peptide and is generally well-tolerated in preclinical studies. As a growth factor peptide, it has a favorable safety profile with minimal toxicity at therapeutic doses. Standard in vitro cytotoxicity assays in osteoblast cell lines are typically performed alongside efficacy studies to rule out nonspecific toxicity. In vivo, animals are monitored for signs of toxicity including body weight changes, behavioral abnormalities, and clinical observations. Comprehensive toxicological characterization including genotoxicity and repeated-dose toxicity studies has not been extensively reported in the public domain. OGP is not approved for human use and is strictly intended for research purposes. The peptide's naturally occurring presence in the body suggests a favorable safety profile, but therapeutic development would require extensive safety evaluation in accordance with regulatory guidelines.
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| References |
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| Additional Infomation |
Osteogenic Growth Peptide (OGP) is a short, naturally occurring 14-mer growth factor peptide found in mammalian serum at micromolar concentrations. It plays a key role in the systemic osteogenic response to local bone marrow injury and regulates osteoblast proliferation, differentiation, and matrix mineralization. The active portion of OGP, the OGP(10-14) region (Tyr-Gly-Phe-Gly-Gly), is cleaved from the full-length peptide and binds to the OGP receptor, activating MAP kinase, Src, and RhoA signaling pathways. OGP has been studied for its potential in bone regeneration and the treatment of osteoporosis. The peptide has a molecular weight of approximately 1.5 kDa. OGP is not in clinical trials and has not received regulatory approval for any indication. It is available from research chemical suppliers for non-clinical research purposes only. OGP is a valuable research tool for studying bone biology and developing new therapies for bone disorders.
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| Molecular Formula |
C68H111N23O17
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| Molecular Weight |
1522.75284
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| Exact Mass |
1522.836
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| CAS # |
132996-61-3
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| PubChem CID |
25079049
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.44g/cm3
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| LogP |
2.407
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| Hydrogen Bond Donor Count |
23
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| Hydrogen Bond Acceptor Count |
22
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| Rotatable Bond Count |
51
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| Heavy Atom Count |
108
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| Complexity |
3030
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| Defined Atom Stereocenter Count |
11
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| SMILES |
CC(C[C@H](NC([C@@H](N)C)=O)C(N[C@H](C(N[C@H](C(N[C@H](C(NCC(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(NCC(N[C@H](C(NCC(NCC(O)=O)=O)=O)CC1=CC=CC=C1)=O)=O)CC2=CC=C(O)C=C2)=O)CC(C)C)=O)[C@H](O)C)=O)CCCNC(N)=N)=O)=O)CCC(N)=O)=O)CCCNC(N)=N)=O)CCCCN)=O)C
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| InChi Key |
VNTJGCYVIRTGMZ-PXGLAOGESA-N
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| InChi Code |
InChI=1S/C68H110N22O18/c1-36(2)28-47(87-57(99)38(5)70)64(106)85-44(16-10-11-25-69)61(103)84-45(18-13-27-77-68(74)75)62(104)86-46(23-24-51(71)93)58(100)80-33-53(95)82-43(17-12-26-76-67(72)73)63(105)90-56(39(6)91)66(108)89-48(29-37(3)4)65(107)88-50(31-41-19-21-42(92)22-20-41)60(102)81-34-54(96)83-49(30-40-14-8-7-9-15-40)59(101)79-32-52(94)78-35-55(97)98/h7-9,14-15,19-22,36-39,43-50,56,91-92H,10-13,16-18,23-35,69-70H2,1-6H3,(H2,71,93)(H,78,94)(H,79,101)(H,80,100)(H,81,102)(H,82,95)(H,83,96)(H,84,103)(H,85,106)(H,86,104)(H,87,99)(H,88,107)(H,89,108)(H,90,105)(H,97,98)(H4,72,73,76)(H4,74,75,77)/t38-,39+,43-,44-,45-,46-,47-,48-,49-,50-,56-/m0/s1
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| Chemical Name |
2-[[2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-aminopropanoyl]amino]-4-methylpentanoyl]amino]hexanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-5-oxopentanoyl]amino]acetyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-hydroxybutanoyl]amino]-4-methylpentanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]acetyl]amino]-3-phenylpropanoyl]amino]acetyl]amino]acetic acid
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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) |
H2O : ~100 mg/mL (~65.63 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 | 0.6567 mL | 3.2835 mL | 6.5671 mL | |
| 5 mM | 0.1313 mL | 0.6567 mL | 1.3134 mL | |
| 10 mM | 0.0657 mL | 0.3284 mL | 0.6567 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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